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BVS 611 Slide Deck II

BVS 611 Slide Deck II. Which of the following insulin products is a short-acting insulin? a.) insulin aspart b.) insulin glargine c.) insulin detemir

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Page 1: BVS 611 Slide Deck II. Which of the following insulin products is a short-acting insulin? a.) insulin aspart b.) insulin glargine c.) insulin detemir

BVS 611 Slide Deck II

Page 2: BVS 611 Slide Deck II. Which of the following insulin products is a short-acting insulin? a.) insulin aspart b.) insulin glargine c.) insulin detemir

Which of the following insulin products is a short-acting insulin?

a.) insulin aspart

b.) insulin glargine

c.) insulin detemir

d.) NPH insulin

Which of the following is a potential consequence of diabetes-related gastroparesis?

a.) increased risk of myocardial infarction

b.) decreased immunocompetence

c.) speeding up hepatic metabolism of orally-ingested drugs

d.) slowing the absorption of orally-ingested drugs

Page 3: BVS 611 Slide Deck II. Which of the following insulin products is a short-acting insulin? a.) insulin aspart b.) insulin glargine c.) insulin detemir

BVS 611 – Pharmacology I

8. Medications for Diabetes

Drug Use Mechanism of Action

Adverse Effects Admin/PK Comments

Glyburide (Micronase®, DiaBeta®)

Type-2 diabetes

Sulfonylurea agent. Stimulates acute release of insulin from functional beta cells. May increase insulin sensitivity in target cells.

Hypoglycemia, wt.gain, hepatic & renal complications blood dyscrasias, GI disturbances, headache, increased cardiac risk in those with CV disease.

Patient monitored for hepatic and renal function. Doses are reduced in elderly patients.

Ocular side effects include blurred vision and changes in accommo-dation. Best effect as monotherapy is approx. 1.5% reduction in A1C.

D:D intrx c/ some SOP meds

Glipizide(Glucotrol®, Glucotrol XL ®)

Type-2 diabetes

Sulfonylurea agent. Stimulates acute release of insulin from functional beta cells. May increase insulin sensitivity in target cells.

Hypoglycemia, wt.gain, hepatic & renal complications blood dyscrasias, GI disturbances, headache, increased cardiac risk in those with CV disease.

Patient monitored for hepatic and renal function. Doses are reduced in elderly patients.

Ocular side effects include blurred vision and changes in accommo-dation. Best effect as monotherapy is approx. 1.5% reduction in A1C. D:D intrx c/ some SOP meds

Other medications:

Page 4: BVS 611 Slide Deck II. Which of the following insulin products is a short-acting insulin? a.) insulin aspart b.) insulin glargine c.) insulin detemir

BVS 611 – Pharmacology I

8. Medications for Diabetes

Drug Use Mechanism of Action

Adverse Effects Admin/PK Comments

Glimepiride (Amaryl®)

****

Type-2 diabetes

Sulfonylurea agent. Stimulates acute release of insulin from functional beta cells. May increase insulin sensitivity in target cells.

Hypoglycemia, wt.gain, hepatic & renal complications blood dyscrasias, GI disturbances, headache, increased cardiac risk in those with CV disease.

Patient monitored for hepatic and renal function. Doses are reduced in elderly patients.

Ocular side effects include blurred vision and changes in accommo-dation. Best effect as monotherapy is approx. 1.5% reduction in A1C. D:D intrx c/ some SOP meds

Acarbose(Precose®)

Type-2 diabetes

Inhibits breakdown of complex starches to glucose, slows absorption of glucose into the bloodstream

Flatulence, diarrhea, abdominal pain. Should not cause hypoglycemia when used as monotherapy. If it occurs, treat with oral glucose instead of table sugar (sucrose.)

Caution is used when the drug is administered with other medications that lower blood glucose due to increased risk of hypo- glycemia.

Best effect as an adjunct is approx. 0.5 – 0.8% reduction in A1C. Not used as monotherapy.

Other medications:

Page 5: BVS 611 Slide Deck II. Which of the following insulin products is a short-acting insulin? a.) insulin aspart b.) insulin glargine c.) insulin detemir

BVS 611 – Pharmacology I

8. Medications for Diabetes

Drug Use Mechanism of Action

Adverse Effects Admin/PK Comments

Miglitol(Glyset®)

Type-2 diabetes

Inhibits breakdown of complex starches to glucose, slows absorption of glucose into the bloodstream

Flatulence, diarrhea, abdominal pain. Should not cause hypoglycemia when used as monotherapy. If it occurs, treat with oral glucose instead of table sugar (sucrose.)

Caution is used when the drug is administered with other medications that lower blood glucose due to increased risk of hypo- glycemia.

Renal function should be monitored. Best effect as an adjunct is approx. 0.5 – 0.8% reduction in A1C. Not used as monotherapy.

Other medications:

Page 6: BVS 611 Slide Deck II. Which of the following insulin products is a short-acting insulin? a.) insulin aspart b.) insulin glargine c.) insulin detemir

BVS 611 – Pharmacology I

8. Medications for Diabetes

Drug Use Mechanism of Action

Adverse Effects Admin/PK Comments

Metformin(Glucophage®,Glucophage XR®, Fortamet®)

****

Type-2 diabetes

Potentiates the effect of endogenous insulin. May work by decreasing hepatic glucose production and improving insulin sensitivity.

N/V/D, flatulence, rash, weakness, headache, hypoglycemia, lactic acidosis, myalgia, blood dyscrasias, chest discomfort, etc.

Caution is used when the drug is administered with other medications that lower blood glucose due to increased risk of hypo- glycemia.

Renal function should be monitored. The drug may be DC’d in renal dysfunction.

Medication is held before surgeries and use of contrast media. Best effect is 1 - 2% reduction in A1C. D:D intrx c/ some SOP meds

Other medications:

Page 7: BVS 611 Slide Deck II. Which of the following insulin products is a short-acting insulin? a.) insulin aspart b.) insulin glargine c.) insulin detemir

BVS 611 – Pharmacology I

8. Medications for Diabetes

Drug Use Mechanism of Action

Adverse Effects Admin/PK Comments

Pioglitazone(Actos®)

****

Type-2 diabetes

Decreases insulin resistance at peripheral sites and in the liver.

Caution in patients with edema or heart failure due to fluid retention. Avoid in hepatic impairment (liver function should be monitored.) Can cause edema, weight gain, induce CHF, tooth disorders, headache, myalgia, sinusitis, anemia.

Can contribute to hypoglycemia when used with other agents that lower blood glucose.

Rare reports of decreased visual acuity, macular edema (new onset or worsening.) Best effect is approx. 0.5 -1.4% reduction in A1C. Used for monotherapy and in combination with other medications.

D:D intrx c/ trimethoprim

Other medications:

Page 8: BVS 611 Slide Deck II. Which of the following insulin products is a short-acting insulin? a.) insulin aspart b.) insulin glargine c.) insulin detemir

BVS 611 – Pharmacology I

8. Medications for Diabetes

Drug Use Mechanism of Action

Adverse Effects Admin/PK Comments

Rosiglitazone(Avandia®)

Type-2 diabetes

Decreases insulin resistance at peripheral sites and in the liver.

Caution in patients with edema or heart failure due to fluid retention. Avoid in hepatic impairment (liver function should be monitored.) Can cause edema, weight gain, induce CHF, tooth disorders, headache, myalgia, sinusitis, anemia.

Used as monotherapy or in combination with other hypoglycemic agents. Can contribute to hypoglycemia when used with other agents that lower blood glucose.

Decreased visual acuity and macular edema have been reported. Best effect is approx. 0.5 -1.4% reduction in A1C. Used for monotherapy and in combination with other medications.

D:D intrx c/ trimethoprim

Other medications:

Page 9: BVS 611 Slide Deck II. Which of the following insulin products is a short-acting insulin? a.) insulin aspart b.) insulin glargine c.) insulin detemir

BVS 611 – Pharmacology I

8. Medications for Diabetes

Drug Use Mechanism of Action

Adverse Effects Admin/PK Comments

Nateglinide(Starlix®)

Type-2 diabetes

Stimulates the release of insulin from functioning beta cells.

Hepatic function impairment can occur. Can cause hypoglycemia, and other adverse effects.

Not used as monotherapy in patients inadequately controlled with other diabetes medications.

Medications which increase blood glucose levels may lessen the effects of nateglinide. Best effect is approx. 0.5 -1.5% reduction in A1C. Usually used in combination other medications.

Repaglinide(Prandin®)

Type-2 diabetes

Stimulates the release of insulin from functioning beta cells.

Hepatic function impairment can occur. Can cause hypoglycemia and many other adverse effects including blood dyscrasias, blood pressure changes, cardiac complications, etc.

Not used as monotherapy in patients inadequately controlled with other diabetes medications.

Medications which increase blood glucose levels may lessen the effects of repaglinide. Best effect is approx. 0.5 -1.5% reduction in A1C. Usually used in combination other medications.

Other medications:

Page 10: BVS 611 Slide Deck II. Which of the following insulin products is a short-acting insulin? a.) insulin aspart b.) insulin glargine c.) insulin detemir

BVS 611 – Pharmacology I

8. Medications for Diabetes

Drug Use Mechanism of Action

Adverse Effects Admin/PK Comments

Exenatide(Byetta®)

(New on the market is Liraglutide (Victoza®)

Type-2 diabetes

Glucagon-like peptide to improve pancreatic beta cell response, moderate glucagon secretion and slow gastric emptying.

Avoided in patients with renal insufficiency, severe GI disease, or gastroparesis. reports of pancreatitis. Can also cause dizziness, diarrhea, GI upset, headache, GERD, hypoglycemia, etc.

Adjunct in the treatment of patients who take metformin, a sulfonylurea, or combination of these meds but who have not achieved adequate control.

Not an insulin substitute. Best effect is approx. 1% reduction in A1C. Given subcutaneously

Pramlintide(Symlin®)

Adjunct in type-1 and type 2 diabetes

Slows rate of food absorp tion,modulates gastric empty-ing. Helps prevent post-meal rise in blood glucose and increases satiety.

N/V, abdominal pain, arthralgia, cough, headache, hypoglycemia, fatigue, dizziness, etc.

Contraindicated in patients with gastroparesis

Doses of other diabetes drugs must be adjusted. Best effect is approx. 0.5% reduction in A1C. Given subcutaneously

Other medications:

Page 11: BVS 611 Slide Deck II. Which of the following insulin products is a short-acting insulin? a.) insulin aspart b.) insulin glargine c.) insulin detemir

BVS 611 – Pharmacology I

8. Medications for Diabetes

Drug Use Mechanism of Action

Adverse Effects Admin/PK Comments

Sitagliptin(Januvia®)

New on the market is Saxagliptin (Onglyza®)

Adjunct in the treatment of type-2 diabetes

Inhibits dipeptidyl peptidase (DPP-4), an enzyme that breaks down incretin hormones. Increases in incretins leads to a rise in insulin levels and a corresponding decrease in blood glucose levels.

Upper respiratory tract infections, sore throat, diarrhea, N/V, hypoglycemia, weight gain, headache, rash, pancreatitis, etc.

Can contribute to hypoglycemia when used with other agents that lower blood glucose, but is used as an adjunct with other medications. It is therefore important to monitor blood glucose levels.

Recent reports of pancreatitis associated with CLASS may affect new entrants and use. Best effect is approx. 0.5 -0.8% reduction in A1C.

Other medications:

Page 12: BVS 611 Slide Deck II. Which of the following insulin products is a short-acting insulin? a.) insulin aspart b.) insulin glargine c.) insulin detemir

BVS 611 – Pharmacology I

9. Respiratory Medications

Drug Use Mechanism of Action

ADEs Administration/PK

Comments

Albuterol (Ventolin®, Proventil®)

****

Asthma, COPD, emphysema, etc.

Β2 adrenergic receptor agonist causes bronchodilation

Vasodilation, tachycardia, palpitations, tremor, CNS stimulation, etc.

Onset of action after inhalation = <15 min. PO and INH products available. Duration approx. 4 hours.

Drug of choice for acute asthma symptoms and to prevent effort-associated asthma.

Levalbuterol (Xopenex®)

Asthma, COPD, emphysema, etc.

Β2 adrenergic receptor agonist causes bronchodilation

Vasodilation, tachycardia, palpitations, tremor, CNS stim.,etc. Can cause atrial fibrillation if used too often in elderly.

INH form only. Longer duration of action, best for maintenance.

Should only be used every 6 – 8 hours.

Pirbuterol (Maxair®)

Asthma, COPD, emphysema, etc.

Β2 adrenergic receptor agonist causes bronchodilation

Vasodilation, tachycardia, palpitations, tremor, CNS stimulation, etc.

INH form only. Duration is 4-6 hours.

Page 13: BVS 611 Slide Deck II. Which of the following insulin products is a short-acting insulin? a.) insulin aspart b.) insulin glargine c.) insulin detemir

BVS 611 – Pharmacology I

9. Respiratory Medications

Drug Use Mechanism of Action

ADEs Administration/PK

Comments

Bitolterol

(Tornalate®)

Asthma, COPD, emphysema, etc.

Β2 adrenergic receptor agonist causes bronchodilation

Vasodilation, tachycardia, palpitations, tremor, CNS stimulation, etc.

INH form only. Duration is 4-6 hours.

Salmeterol (Serevent®)

Maintenance in chronic asthma, COPD, etc.

Long acting Β2 adrenergic receptor agonist

Vasodilation, tachycardia, palpitations, tremor, CNS stimulation, nasopharyn- gitis, HA, cough, etc.

INH form only, duration is 12 hours, so drug is only used twice a day.

Not for acute attacks. Advair Advair DiskusDiskus®® is a combination of salmeterol and fluticasone.

Ipratropium (Atrovent®)

Bronchospasm associated with COPD in adults.

Muscarinic antagonist, reverses acetylcholine-induced bronchospasm.

Cough, dry mouth and blurred vision can occur.

INH form only. Usually used every 6 hours.

Caution in narrow angle glaucoma.

Page 14: BVS 611 Slide Deck II. Which of the following insulin products is a short-acting insulin? a.) insulin aspart b.) insulin glargine c.) insulin detemir

BVS 611 – Pharmacology I

9. Respiratory Medications

Drug Use Mechanism of Action

ADEs Admin/PK Comments

Tiotropium (Spiriva®)

****

Bronchospasm associated with COPD in adults, maintenance use.

Muscarinic antagonist, reverses acetylcholine-induced bronchospasm.

Cough, dry mouth, blurred vision can occur.

INH form only. Usually used once daily.

Caution in narrow angle glaucoma.

Theophylline, aminophylline products

Maintenance therapy in moderate – severe asthma, no longer first line therapy.

Exact mechanism is unknown, may inhibit enzyme which mediates broncho-dilation

N/V, headache, insomnia, tachycardia, dizziness, agitation, seizures, etc.

Usually given in PO or IV form. Several drug:drug interactions are possible. Avoid use.

Rarely used. Not recommended for patients with seizure disorders, CV disease or PUD.

Cromolyn (Intal®), Nedocromil (Tilade®)

Prophylaxis of asthma attacks; maintenance therapy only.

Mast cell stabilizers prevent release of histamine.

Minimal ADEs, throat irritation and unpleasant taste reported.

Inhalant form. May take several weeks for full effect to occur.

Not effective in treating acute attacks.

Page 15: BVS 611 Slide Deck II. Which of the following insulin products is a short-acting insulin? a.) insulin aspart b.) insulin glargine c.) insulin detemir

BVS 611 – Pharmacology I

9. Respiratory Medications

Drug Use Mechanism of Action

ADEs Admin/PK Comments

Systemic corticosteroids (prednisone prednisone ****,,

methylprednis-olone, etc.)

Acute asthma and COPD exacer-bation

Decrease inflammation and edema in respiratory tract, enhance sympathomi-metic bronchodilator activity.

Na+/water retention, elevate blood glucose levels, can alter electrolytes, GI irritation, CNS effects, can effect WBC count. Several long-term use consequences.

PO/IV/IM administra- tion.

Adjuncts in acute situations not able to be controlled with bronchodilators alone. Taper as soon as possible to avoid adrenal reliance. Use increases IOP; caution in glaucoma; cataracts

Flunisolide (Aerobid)

Chronic asthma (main-tenance)

Decrease inflammation and edema in respiratory tract, enhance sympathomi-metic bronchodilator activity.

Usually does not cause systemic corticosteroid effects. Increased risk of oral candidiasis.

Some potential for drug interactions.

Inhalant form

Similar products: beclomethasone (QVAR®), mometasone (Asmanex®), triamcinolone (Azmacort®) Use can increase IOP; caution in glaucoma; cataracts.

Page 16: BVS 611 Slide Deck II. Which of the following insulin products is a short-acting insulin? a.) insulin aspart b.) insulin glargine c.) insulin detemir

BVS 611 – Pharmacology I

9. Respiratory Medications

Drug Use Mechanism of Action

ADEs Admin/PK Comments

Fluticasone (Flovent)

Chronic asthma (maintenance)

Decrease inflammation and edema in respiratory tract, enhance sympathomi-metic bronchodilator activity.

Usually does not cause systemic corticosteroid effects. Increased risk of oral candidiasis. Some potential for drug interactions.

INH form Similar to products above. Use can increase IOP; caution in glaucoma; cataracts.

Montelukast (Singulair®),

Zafirlukast (Accolate®),

Zileuton (Zyflo CR®)

Chronic asthma prevention / maintenance

Leukotriene receptor antagonists

HA, GI upset. May cause hepatic ADEs. Some drug:drug interactions. New CNS/Psych warnings.

PO forms. Montelukast taken once daily, zafirlukast and zileuton taken BID.

Watch for increased respiratory infections in elderly patients.

Page 17: BVS 611 Slide Deck II. Which of the following insulin products is a short-acting insulin? a.) insulin aspart b.) insulin glargine c.) insulin detemir

BVS 611 – Pharmacology I

10. Anti-infective Medications

Introduction to Anti-infectives

Microorganisms are living forms of microscopic or submicroscopic size. General groups include:

- Bacteria (includes Chlamydiae, Rickettsiae, and Mycoplasma)- Viruses- Fungi- Protozoa

Bacteria are single-celled microorganisms occurring in many forms, existing either as free-living organisms, or as parasites (as in the case of obligate intracellular parasites such as Chlamydiae.) Bacteria have a range of biochemical and often pathogenic properties. Bacteria are generally small, with a size ranging from 0.2 to 2 microns.

Bacteria are often initially divided into two general groups based on their response to the Gram’s stain procedure:

Gram PositiveGram Positive Gram NegativeGram Negative

After the cell sample is fixed, stained, and washed, the bacterial cell walls retain the crystal violet dye, or remain stained. These bacteria have a purple cell wall when viewed under the microscope.

After the cell sample is fixed, stained, and washed, the bacterial cell walls do not retain the crystal violet dye. (They retain the reddish safranin dye.) These bacteria are decolorized, and have a light reddish cell wall when viewed under the microscope.

Page 18: BVS 611 Slide Deck II. Which of the following insulin products is a short-acting insulin? a.) insulin aspart b.) insulin glargine c.) insulin detemir

BVS 611 – Pharmacology I

10. Anti-infective Medications

Bacteria are not always able to be fully identified by Gram’s stain alone. Other special stains and dyes may be needed to give a preliminary or final identification of the bacteria:

- Acid fast staining (used for Mycobacteria) is one example.

Some bacteria are not able to be identified by use of the Gram’s stain since they do not possess a rigid cell wall. Such bacteria may be identified on the basis of rising antibody titers, special immunofluorescence assays, etc. - Legionella (i.e. Legionella pneumophilia) - Rickettsiae (i.e. Rickettsia rickettsiae) - Chlamydia (i.e. Chlamydia pneumonia, C. trachomatis, C. psittaci) - Mycoplasma (i.e. Mycoplasma pneumoniae)

The principal groups of true bacteria are distinguished by their morphologic shapes when viewed under a microscope:

- Cocci: Spherical. Examples are Streptococci, Staphylococci, and Neisseria

- Bacilli: Rod-shaped. Examples are E. coli, Bacillus, and Clostridia

- Spirillum: Short, rigid spirals. An example is Vibrio

- Spirochetes: Protozoa-like bacteria that are thin, flexible, motile, and spiral-shaped. Examples are Borrelia and Treponema

- Fungus-like: Bacteria that possess branching filamentous elements resembling fungal hyphae. Examples are Mycobacteria, Nocardia, and Actinomyces

Page 19: BVS 611 Slide Deck II. Which of the following insulin products is a short-acting insulin? a.) insulin aspart b.) insulin glargine c.) insulin detemir

- Rickettsiae: Extremely small parasitic bacteria once thought to be viruses because their growth takes place within a host cell. Rickettsiae do possess a cell wall and other bacterial elements. Examples are Coxiella, Typhus and Rickettsia. Not routinely seen on

Gram’s stain.

- Mycoplasma: Very small bacteria that lack a rigid cell wall. Mycoplasma bacteria are bound by unit membranes, so are not seen on routine Gram’s stain. They are usually diagnosed on the basis of rising antibody titers. An example is Mycoplasma pneumoniae.

- Chlamydia: Smaller than Rickettsiae, these bacteria were also once thought to be viruses. Chlamydia are obligate intracellular parasites which do possess cell walls and ribosomes, but must rely on the intracellular processes of the host cell to produce metabolic energy. Not routinely seen on Gram’s stain, Chlamydia are often diagnosed using titers. Examples are Chlamydia pneumoniae, C. trachomatis, and C. psittaci.

- Viruses are the smallest microorganisms known to have pathogenic properties in humans. The size of these microorganisms can be in nanomicrons. Viruses commonly consist of a nucleic acid fragment (DNA or RNA) core, a capsid, and a lipoprotein coat. Viruses generally use the structures and systems in host cells to replicate themselves. Viruses most

often involved in causing eye infections include the herpes viruses, and adenoviruses.

BVS 611 – Pharmacology I

10. Anti-infective Medications

Page 20: BVS 611 Slide Deck II. Which of the following insulin products is a short-acting insulin? a.) insulin aspart b.) insulin glargine c.) insulin detemir

Terminology Review

Along with initial patient assessment, identification of the pathogen(s) is critical in determining the most appropriate therapy for bacterial infection. Visual appearance/characteristics and laboratory analysis of specimens are very important.

SPECIMEN COLLECTION: Specimens should be collected with care to prevent inadvertent contamination. Specimen collection sites should represent the suspected location of infection. Specimen amount should be of sufficient size and numbers. Specimens need to be placed in appropriate containers, and labeled carefully. Delivery to the Laboratory should occur promptly.

CULTURE AND SENSITIVITY: A test in which patient specimens are cultured on appropriate media and incubated. Bacteria which have grown on the media are directly isolated, identified, and tested for susceptibility to different antibiotics. Sensitivity testing may be done by using the disc method, automated disc method, or by serial dilution method.

BVS 611 – Pharmacology I

10. Anti-infective Medications

Page 21: BVS 611 Slide Deck II. Which of the following insulin products is a short-acting insulin? a.) insulin aspart b.) insulin glargine c.) insulin detemir

CULTURES: An example: A Gram’s stain reveals Gram + cocci in chains and pairs. On culturing the bacteria on a blood agar plate, the following may be seen:

Colonies surrounded by greenish zones = partially hemolytic bacteria = Alpha hemolytic Streptococci such as S. viridans, or S. pneumoniae

Colonies surrounded by clear zones = fully hemolytic bacteria = Beta hemolytic Streptococci such as Group A Streptococci

Colonies not surrounded by zones = non- hemolytic bacteria = Gamma hemolytic Streptococci such as Enterococci.

BVS 611 – Pharmacology I

10. Anti-infective Medications

Page 22: BVS 611 Slide Deck II. Which of the following insulin products is a short-acting insulin? a.) insulin aspart b.) insulin glargine c.) insulin detemir

BVS 611 – Pharmacology I

10. Anti-infective Medications

SENSITIVITY: An example:

Disc sensitivity testing: Discs containing different antibiotics and/or different concentrations of antibiotics are placed on a growth medium that has been colonized with the cultured bacteria. After incubation, areas of inhibited bacterial colony growth are assessed. Wide zones of inhibited (no) growth indicate antibiotic sensitivity. Areas with minimal growth inhibition indicate minimal antibiotic sensitivity. Areas of no growth inhibition indicate antibiotic resistance.

SENSITIVE MINIMALLY RESISTANT SENSITIVE

Other methods of assessing antimicrobial resistance and sensitivity include serial dilution testing.

Page 23: BVS 611 Slide Deck II. Which of the following insulin products is a short-acting insulin? a.) insulin aspart b.) insulin glargine c.) insulin detemir

BVS 611 – Pharmacology I

10. Anti-infective Medications

MINIMUM INHIBITORY CONCENTRATION (MIC): The lowest in-vitro concentration of antibiotic in solution with a bacterial suspension that prevents/inhibits growth of the bacteria after an incubation period.

- If the concentration of antibiotic represented by the MIC can be achieved in the patient’s serum by normal routes of delivery, the bacteria is said the be sensitive to

the antibiotic.

- If the MIC is above the achievable level, or is within a range that would be toxic to a patient, then the bacteria is said to be resistant to the antibiotic.

Susceptibility and resistance are functions of the site of infection, the bacteria, and the antibiotic being tested..

BROAD SPECTRUM: Antibiotics which halt the growth of, or eradicate many different bacteria.

NARROW SPECTRUM: Antibiotics which are effective for very specific bacteria only.

Page 24: BVS 611 Slide Deck II. Which of the following insulin products is a short-acting insulin? a.) insulin aspart b.) insulin glargine c.) insulin detemir

BVS 611 – Pharmacology I

10. Anti-infective Medications

BACTERIOCIDAL: Antibiotics whose mechanisms of action usually result in bacterial cell death.

BACTERIOSTATIC: Antibiotics whose mechanism of action usually result in inhibiting or arresting the growth, development, or multiplication of the infecting bacteria.

VIRUSTATIC (Virucidal): Not commonly used terms. “Anti-viral” is the more common term, since causing outright pharmacologic eradication of the infecting virus is sometimes not possible.

Anti-infective Mechanisms of Action

Most anti-infectives work by one or more of the following mechanisms:1. Inhibition of cell wall synthesis, cause cell wall lysis (Penicillins, cephalosporins, vancomycin, (daptomycin))2. Alteration of cell membrane permeability, inhibition of active transport across the cell

membrane (Most antifungals)3. Inhibition of protein synthesis via inhibition of ribosomal subunit transcription/translation

(Macrolides/ketolides, tetracyclines, glycylcyclines, (daptomycin), quinu/dalfo, aminoglycosides, clindamycin, linezolid)

4. Inhibition of nucleic acid synthesis/replication, stimulating reduction products (Sulfonamides, metronidazole, possibly tinidazole)

5. Inhibition of DNA-gyrase or DNA-polymerase (Fluoroquinolones)6. Binding to DNA, interfering with/preventing replication (Most antiviral agents)

Page 25: BVS 611 Slide Deck II. Which of the following insulin products is a short-acting insulin? a.) insulin aspart b.) insulin glargine c.) insulin detemir

BVS 611 – Pharmacology I

10. Anti-infective Medications

Considerations in Selecting Appropriate Antimicrobial Agents

1. The infecting microorgansim and its susceptibilities

2. The type of infection: abscess, UTI, sepsis, meningitis, cellulitis, etc.

3. Host factors: age, current illnesses, immune status, renal function, allergies, other medications, WBC count, etc.)

4. Anti-infectives and their properties: dose, routes of administration, metabolic properties, where the drug is excreted, protein binding, tissue penetration capabilities, potential toxicities, potential drug interactions, therapeutic serum concentration levels, etc.

5. Public health considerations: hospital and community resistance patterns.

Page 26: BVS 611 Slide Deck II. Which of the following insulin products is a short-acting insulin? a.) insulin aspart b.) insulin glargine c.) insulin detemir

Reminder

BVS 611 – Pharmacology I

10. Anti-infective Medications

Antibiotics are primarily effective against bacteria. They do not have clinical effect against viruses. Antibiotics are also not effective at treating fungal infections. Antifungal medications are needed to treat

these infections. Some antibiotics also have anti-protozoal properties and can be used to treat infections caused by some

protozoa. Final identification and susceptibilities of the bacteria to anti-infective agents come from culture and

sensitivity testing. Viral infections are commonly diagnosed empirically, but special tests such as immunofluorescent

assays or serum titer analysis may be used in some cases of serious or systemic illness.

Most Common Infections of the Eye

Blepharitis Hordeolum Conjunctivitis (Bacterial and Viral) Keratitis (Bacterial and Viral) Dacryocystitis Canaliculitis Endophthalmitis Retinitis Orbital cellulitis

Page 27: BVS 611 Slide Deck II. Which of the following insulin products is a short-acting insulin? a.) insulin aspart b.) insulin glargine c.) insulin detemir

Common Pathogenic Bacteria

GRAM POSITIVE

RODS COCCI

AEROBIC ANAEROBIC ANAEROBICAEROBIC

1. Listeria ¤

2. Bacillus

- anthracis

- cereus ¤

- other species

1. Clostridium

- perfringens

- difficile

- tetani

- botulinum

2. Diphtheroids

- C.diphtheriae

- P. acnes¤

1.Peptostreptococcus

2. Peptococcus

Chains Clusters

(Hemolysis) (Coagulase)

+ -

Staphy lococcus

- aureus¤

(MSSA,

MRSA)

Staphy lococcus

- epidermidis ¤

- saprophy ticus

Alpha Beta Gamma

1. Streptococcus

pneumoniae ¤

2. Streptococcus

viridans¤

1. Group A (Strep.

pyogenes ¤)

2. Group B

3. Group C

4. Group E

5. Group F

6. Group G

Group D

Non- Enterococcus

Enterococcus -Strep.faecalis

-Strep.faecium

¤ = Organisms causing infections o f the eye

Page 28: BVS 611 Slide Deck II. Which of the following insulin products is a short-acting insulin? a.) insulin aspart b.) insulin glargine c.) insulin detemir

Common Pathogenic Bacteria

GRAM NEGATIVE

RODS COCCI

AEROBIC ANAEROBIC ANAEROBICAEROBIC

1. E. coli ¤

2. Shigella ¤

3. Salmonella

- typhi

- non-typhi ¤

4. Klebsiella ¤

5. Enterobacter ¤

6. Serratia ¤

7. Proteus ¤

8. Morganella

9. Providencia ¤

10. Yersinia ¤

11. Citrobacter ¤

12. Pseudomonas ¤

13. Vibrio

14. Hemophilus (influenzae ¤)

15. Legionella

16. Helicobacter

17. Pasturella

18. Bordetella

19. Stenotrophomonas

20. Aeromonas

1. Bacteroides

- fragilis

- bivius

- melaninogenicus

2. Fusobacterium ¤

1. Neisseria

- N. gonorrheae ¤

- N. meningitidis ¤

2. Moraxella

- M. catarrhalis ¤

1. Eikenella

2. Veillonella

¤ = Organisms commonly seen in infections of the eye

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Other Eye Infection Pathogens

Bacterial:

Chlamydia trachomatis

Actinomyces

Nocardia

Fungal:

Candida sp.

Aspergillus

Parasitic:

Acanthamoeba

Viruses:

Herpes viruses:

Herpes simplex type 1

Herpes simplex type 2

Varicella-zoster

Cytomegalovirus

Adenoviruses:

Types 3 and 7 in children

Ttypes 8, 11 and 19 in adults

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BVS 611 – Pharmacology I

10. Anti-infective Medications

Matching infection with the etiology

CONDITION COMMON ETIOLOGY

Blepharitis Staphyloccocus aureus, Staphylococcus epidermidis, seborrhea, dry eye, rosacea

Hordeolum External: Staphylococcus aureus

Internal (Meibomian glands, can be acute, subacute or chronic): Staphylococcus aureus, MRSA (CA or HA)

Bacterial Conjunctivitis

Staphylococcus aureus, N. gonorrheae, C. trachomatis, Streptococcus pneumoniae, Hemophilus influenzae

Viral Conjunctivitis Adenovirus (types 3 and 7 in children and types 8,11, and 19 in adults), Herpes simplex types 1 & 2

Bacterial Keratitis Pseudomonas aeruginosa, Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Group A Streptococcus (S. pyogenes), Enterobacteriaceae, Listeria, Hemophilus sp. Mycobacterium chelonae post refractive eye surgery.

Viral Keratitis Herpes simplex types 1 & 2, Varicella-zoster virus

Fungal Keratitis Aspergillus, Fusarium, Candida

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BVS 611 – Pharmacology I

10. Anti-infective Medications

Matching infection with the etiology

CONDITION ETIOLOGY

Protozoan Keratitis Acanthamoeba sp. (Soft contact lens wearers)

Dacryocystitis Pseudomonas aeruginosa, Staphylococcus aureus, Streptococcus pneumoniae, Group A Streptococci (S. pyogenes), Hemophilus influenzae

Canaliculitis Actinomyces, Fusobacterium, Nocardia, Candida sp., etc.

Endophthalmitis Staphylococcus epidemidis, Staphylococcus aureus, streptococci (including S. viridans, pneumoniae), P. acnes, enterococci, gram negative rods (Hemophilus influenzae, Bacillus sp.), N. meningitidis, Candida sp.

Retinitis Varicella zoster, Herpes simplex, Cytomegalovirus

Orbital cellulitis Streptococcus pneumoniae, Hemophilus influenzae, Moraxella catarrhalis, Staphylococcus aureus, anaerobes, Group A Streptococci, gram negative rods

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BVS 611 – Pharmacology I

10. Anti-infective Medications

Penicillins

MOA: Bacteriocidal: inhibit bacterial cell wall synthesis, inhibit bacterial enzymes which assemble peptidoglycan, activate autolysis.

Uses: - Dicloxacillin: Effective against some streptococci and staphylococci. Many bacteria have acquired resistance, limiting its usefulness. Does not work against Pseudomonas. MSSA

may respond. MRSA does NOT. Is available in oral form only.

- Amoxicillin: Effective against some streptococci, staphylococci, and Listeria. Additional effectiveness against a few gram-negative rods and cocci. Many

bacteria have acquired resistance. Is available in oral form only. Does not work against Pseudomonas, MSSA or MRSA.

- Amoxicillin/clavulanate: Clavulanate added to restore effectiveness of amoxicillin against some bacteria that have acquired resistance. Used orally for some streptococci

and staphylococci, some gram-negative rods and cocci. Does not work against Pseudomonas. MSSA may respond. MRSA does NOT.

- Ampicillin: Effective against some streptococci, staphylococci and Listeria. Does not work against Pseudomonas, MSSA or MRSA.

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BVS 611 – Pharmacology I

10. Anti-infective Medications

Penicillins

Adverse Effects and Other Information: Amoxicillin and amoxicillin/clavulanate need to be dose-adjusted in patients with renal impairment. Dicloxacillin may not. Consult a pharmacist for assistance on renal dose adjustments if patient reports kidney problems, renal disease, or renal dialysis on the medical history.

Follow scope of practice recommendations for duration of therapy and for referral. Consult a pharmacist or a drug information center for additional assistance with recommendations for duration of therapy.

Caution in patients with history of allergy to penicillins. Take thorough medication histories. Allergic reactions are a common side effect; can be immediate or delayed and can range from rashes to anaphylaxis. Monitor patients closely. GI effects with oral use have included nausea, vomiting, and diarrhea. CNS effects are rare, but can include confusion, seizures and encephalopathy. (More common in high doses, and in infants/children.) Blood dyscrasias can occur: eosinophilia, thrombocytopenia, rarely leukopenia, neutropenia.

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10. Anti-infective Medications

Cephalosporins MOA: Bacteriocidal: inhibit bacterial cell wall synthesis, inhibit bacterial enzymes which assemble peptidoglycan.

Uses:- Cephalexin and Cefadroxil: Effective against many Gram positive bacteria, not good for

Gram negative bacteria in general. Will not cover anaerobic bacteria, Pseudomonas, or Enterococci. Many bacteria have acquired resistance to these agents. Available in oral form only.

- Cefaclor: Generally the same Gram positive coverage as cephalexin and cefadroxil, has a little more Gram- negative rod coverage. Does not cover enterococci or Pseudomonas. Available in oral form only.

Note: Cefotetan has been re-approved in generic form in the United States. Avoid using or prescribing this cephalosporin in patients taking anticoagulants/blood thinners due to increased risk of bleeding interactions.

Adverse Effects and Other Information: Some cephalosporins may need to be dose adjusted in patients who have renal impairment. Consult a pharmacist for assistance on renal dose adjustments if patients report kidney problems, renal disease or renal dialysis on medical history. Other adverse effects include fatigue, dizziness, vertigo, and headache. Rash and other manifestations of allergic responses are common. Exfoliative dermatitis can rarely occur. Nausea, vomiting and diarrhea are common. Hepatic and renal effects may rarely occur. Blood dyscrasias include eosinophilia, thrombocytopenia, neutropenia, and leukopenia can occur.

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10. Anti-infective Medications

Follow scope of practice recommendations for duration of therapy and for referral. Consult a pharmacist or drug information center for additional assistance with recommendations for duration of therapy.

It is estimated that 2-10% of patients who are allergic to penicillin will also be allergic to cephalosporins. Allergies to cephalosporins may occur in up to 5% of patients. Reactions may range from rash to anaphylaxis. Take careful patient histories.

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BVS 611 – Pharmacology I

10. Anti-infective Medications

Fluoroquinolones MOA: Inhibition of bacterial DNA-gyrase, which interferes with bacterial reproduction. Effects are often bacteriocidal. Most are broad spectrum.

Indications: Some Gram +, many Gram - bacteria. Not good against MRSA, not generally recommended against Enterococci. Most do not adequately cover against Bacteroides, most will cover Chlamydia. Guard against over-use as bacterial resistances are increasing!

Uses: Examples: ciprofloxacin, gatifloxacin, levofloxacin, moxifloxacin, norfloxacin, and ofloxacin. Most ophthalmic solutions used in bacterial conjunctivitis will be used for 7 days. Most solutions used in corneal ulcers/keratitis will be used for 5 – 14 days. Newest addition to the group is besifloxacin (Besivance®).

Adverse Effects and Other Information: Patients who are allergic to one fluoroquinolone can easily cross-react with others. Avoid use in patients with a history of allergy to any fluoroquinolone.

Avoid over-use of fluoroquinolones for conjunctivitis. May cause white precipitate of active drug at the site of epithelial defect that may be confused with a worsening infection.

There are numerous potential drug interactions, adverse effects, and cautions with oral use of fluoroquinolones. In addition, renal dose adjustments are also needed in patients with renal impairment or renal disease who take oral dosage forms. (Not generally needed for ophthalmic forms.) Ophthalmic forms will be preferred for treatment in most cases.

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BVS 611 – Pharmacology I

10. Anti-infective Medications

Fluoroquinolones

Cautions (for ophthalmic preparations): - Use with great caution if at all in patients with seizure history. - Can increase photosensitivity and cause photophobia. - Counsel patients on potential ophthalmic adverse effects: burning/stinging sensation in the eye, blurred vision, redness/irritation in the eye, eye pain, foreign body

sensation, tearing, and/or dry eye. - Rare but potentially serious side effects can include severe exfoliative dermatitis,

severe allergic reactions including anaphylaxis, periocular or facial edema,

dizziness, etc. - Potential caution in patients taking blood-thinning medications.

Oral fluoroquinolones may interact with many other oral medications. Check for potential drug to drug interactions with oral medications before prescribing oral quinolones.

SulfonamidesMOA: Sulfa antibiotics are structural analogs of PABA and competitively inhibit the bacterial enzyme necessary for incorporating PABA into dihydrofolic acid, the folic acid precursor. Inhibiting folic acid formation results in the bacteria not being able to synthesize amino acids and

DNA. Uses: Originally broad spectrum bacteriostatic antibiotics with specific antibacterial and antiprotozoal activities. Acquired bacterial resistances have limited use of this class, although for some uses, this class of drugs is still somewhat medically important. SMX/TMP is currently one of the oral initial agents to consider for CA-MRSA. ODs can prescribe oral SMX/TMP.

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BVS 611 – Pharmacology I

10. Anti-infective Medications

SulfonamidesSulfacetamide sodium ophthalmic solution (10%, 15%, 30%), and 10% ophthalmic

ointment occasionally used for bacterial conjunctivitis. Other agents used primarily for trachoma/chlamydial infections currently. Topical form not a good option for CA-MRSA.

Sulfisoxazole 4% ophthalmic ointment and 4% ophthalmic solution occasionally used for bacterial conjunctivitis. Other agents used primarily for trachoma/chlamydial infections currently. Topical form not a good option for CA-MRSA.

Adverse Effects and Other Information: Can cause stinging and burning on application. Allergic reactions are possible. Potential for cross-reactivity with other sulfa-containing drugs. Dermatologic reactions can range from swelling to hives and rash. Severe exfoliative dermatitis is potentially possible. Products are incompatible with silver-containing preparations.

Polymyxin and BacitracinMOA: Polymyxin is a bactericidal agent that works by binding to cytoplasmic membranes, disrupting the structure and altering membrane permeability. Most effects are against sensitive Gram-negative bacteria. (Polymyxin has no effect against MRSA.) Bacitracin is a bactericidal agent that works by binding to bacterial cell membranes and interfering with cell wall synthesis. Most effects are against sensitive Gram-positive bacteria.

Uses: Both medications have been used singly, and in combination with other anti-infectives (i.e. neomycin) for short-term treatment of external ocular infections caused by susceptible bacteria. Not for long-term treatment. Acquired bacterial resistance has impacted former widespread usage.

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BVS 611 – Pharmacology I

10. Anti-infective Medications

Polymyxin and Bacitracin

Adverse Effects and Other Information: Local adverse effects are possible. Check previous patient sensitivity reactions before usage.

Tetracyclines

MOA: Inhibit bacterial protein synthesis by binding to the 30-S ribosomal subunit. Bacteriostatic effects, variable effects against some Gram-positive bacteria, reliable effects against systemic Listeria infections. Have effects against some specific Gram- negative bacteria including Neisseria meningitidis and Legionella. Are effective against Mycoplasma, Chlamydia, and Rickettsia. Some anti-clostridial activity, though not against C. difficile.

Ophthalmic preparations are no longer available in the U.S.

Uses: Oral use should be rare, and considered for very specific conditions only (chlamydial inclusion conjunctivitis, trachoma). The oral tetracycline group includes doxycycline and tetracycline.

Adverse Effects and Other Information: There are many potential adverse effects and drug interactions possible with use of tetracycline antibiotics. Doctors of Optometry should prescribe these medications sparingly and with caution.

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BVS 611 – Pharmacology I

10. Anti-infective Medications

Tetracyclines

Numerous drug-to-drug and drug-to-food interactions exist. Pharmacists can assist in identifying possible interactions

Photosensitivity is common with these antibiotics.

GI effects: antibiotic-associated pseudomembranous colitis, N/V, abdominal pain, potential pancreatitis, hepatic effects

Allergic reactions are possible. Cross-sensitivity exists between agents in the same class.

Avoid use in pregnancy and in children.

Should very rarely be considered in Optometry practice.

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BVS 611 – Pharmacology I

10. Anti-infective Medications

MacrolidesMOA: Inhibit protein synthesis by binding to 50-S ribosomal subunit. Activity against some Gram-positive bacteria (Group A, B, C, and G Streptococcus, Streptococcus pneumoniae, MSSA, and Listeria) although resistance to many of these bacteria is increasingly a problem. Some activity against specific Gram-negative bacteria (N. meningitidis, M.catarrhalis, H. influenzae, Legionella) Generally very good for Mycoplasma, Chlamydia, Rickettsia and some Clostridia (though not C. difficile.)

Uses: Current California Optometry regulations specify azithromycin is limited to the treatment of eyelid infections and chlamydial disease manifesting in the eyes. Erythromycin 0.5% ophthalmic ointment is still available for superficial ocular infections and neonatal conjunctivitis. Oral clarithromycin and erythromycin should be dose-adjusted in renal impairment. Azithromycin does not need to be dose-adjusted in renal impairment patients. Contact a pharmacist for assistance with dose adjustments, or refer patient.

Adverse Effects and Other Information: Taken orally or parenterally, these drugs can cause some potentially serious side effects:

- Hepatic complications such as hepatitis and jaundice- Renal complications- GI effects can include GI irritation, nausea, vomiting, and diarrhea- Ototoxicity may occur- Allergic reactions. Cross-reactivity between agents in this class is possible. - Allergic reactions can range from mild rash to anaphylaxis.

Numerous potential drug-to-drug interactions exist with erythromycin, clarithromycin and

azithromycin. Check with a pharmacist as needed.Caution in patients taking blood-thinning medications. Monitor for the appearance of super-infection (candidiasis).

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BVS 611 – Pharmacology I

10. Anti-infective Medications

AminoglycosidesMOA: Inhibition of bacterial protein synthesis by binding principally to 30-S and 50-S ribosomal subunits. Aminoglycoside action in bacteria is specifically bacteriocidal, however since these drugs do cause eventual cell death through cytoplasmic membrane disruption. Some limited activity against MSSA, but not generally used against Gram-positive bacteria. Used widely for many Gram–negative bacteria. Little to no activity against atypical bacteria, no anaerobic effects.

Uses: Ophthalmic products include: gentamicin 0.3% ointment and solution, tobramycin 0.3% ointment and solution, and neomycin (in combination with other anti-infectives such as polymyxin, bacitracin, etc. Occasionally used prophylactically, still used in some bacterial conjunctivitis or keratitis cases. Some concern for recently reported bacterial resistances (Streptococcus pneumoniae, Pseudomonas). Patients who do not respond quickly need rapid referral.

Adverse Effects and Other Information: Local irritation can occur with ophthalmic use. Caution in patients with myasthenia gravis as slight potential for neuromuscular junction blockade effects can worsen or exacerbate symptoms. Monitor for appearance of allergic reactions, swelling of eyelids, face, appearance of rash, etc. Dermatologic reactions are rare but possible.

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BVS 611 – Pharmacology I

10. Anti-infective Medications

Antiviral Agents

Trifluridine 1% ophthalmic solution is indicated for use in Herpes simplex-related keratitis and keratoconjunctivitis. It works by incorporating in place of thymidine into viral DNA, weakening the viral ability to infect tissue. It is not indicated for prophylactic use. Trifluridine 1% ophthalmic solution should be kept refrigerated. Can cause hyperemia, epithelial keratopathy, increased intraocular pressure, dry eye, and irritation. Patients should also be warned that it can cause burning or stinging on instillation.

Vidarabine 3% ophthalmic ointment is indicated for use in Herpes simplex-related keratitis and keratoconjunctivitis. It works by inhibiting viral DNA polymerase and prevents lengthening or building of DNA viral chains. It is not indicated for use in treating infections caused by adenoviruses. Can cause local hypersensitivity reactions including itching, redness, foreign body feeling in the eye, swelling, pain, burning or other irritation on application. It can also increase flow of tears. Can cause increased sensitivity of eyes to light. Recommend sunglasses and avoiding prolonged exposure to sunlight. Can be administered with antibiotics and corticosteroids. Can cause small punctate defects in the cornea with too-frequent use.

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BVS 611 – Pharmacology I

10. Anti-infective Medications

Antiviral Agents

Oral acyclovir is listed in the California Optometry scope of practice for treatment of ophthalmic Herpes zoster. Acyclovir works by inhibiting DNA replication and synthesis.

Oral acyclovir should not be taken by patients who are sensitive to valacyclovir. Cross-sensitivity can occur.

Acyclovir can cause renal failure, and can complicate or worsen renal function in patients with renal impairment. Dose adjustments need to be made in renal failure patients. Consult a pharmacist for assistance, or refer patient.

Encephalopathy/neurotoxicity, blood dyscrasias, coagulation problems, hepatic complications, severe skin reactions, visual changes, GI disturbances, agitation, dizziness, myalgia, paresthesias, and other side effects are possible.

The drug must be used with caution and close patient monitoring. Oral doses should be taken with a full glass of water.

Some potentially serious drug–to-drug interactions are possible. Consult with a pharmacist as needed.

Valacyclovir (Valtrex) is a prodrug for acyclovir. MOA is the same as acyclovir. Similar warnings and potential adverse reactions. Valacyclovir has recently been added to scope of practice for doctors of optometry in many states.

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BVS 611 – Pharmacology I

10. Anti-infective Medications

Antiviral Agents

Note: Corticosteroids can accelerate the spread of viral infections and are usually contraindicated in superficial Herpes simplex virus keratitis. Steroids may be used concurrently with trifluridine in the treatment of Herpes simplex stromal infections. In these cases, trifluridine should be continued for a few days after the steroid has been discontinued.

Combination Products

Corticosteroid and anti-infective combinations are sometimes prescribed for steroid-responsive inflammatory conditions with bacterial infections or risk of bacterial infections.

Anti-infective component may consist of sulfacetamide sodium, neomycin/polymyxin, gentamicin, or tobramycin.

Corticosteroid component may consist of prednisone, hydrocortisone, dexamethasone, or prednisolone.

All combination ophthalmic solutions should be shaken well prior to use.

Steroid-containing products can increase intraocular pressure. Select for use, and monitor patients appropriately.

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BVS 611 – Pharmacology I

10. Anti-infective Medications

TYPICAL ADULT ORAL ANTI-INFECTIVE DOSESNote:1. Anti-infective use and dosage should be adjusted as needed on an individual patient

basis, taking into account indication for use, allergy /intolerance status, age, height/weight, functional status of metabolic and elimination systems (as appropriate), C & S results, duration of therapy, potential for drug:drug interactions and adverse effects.

2. Consult a drug information resource, a pharmacist, and/or a drug information center as needed. Always consult a drug information center or pediatrician for pediatric and infant doses, and the physician supervising the pregnancy of expectant women.

3. Trade names listed below reflect ORAL dosage forms/products, not ophthalmic products. The symbol ۩ indicates a medication where the knowledge of generic name, dose, and comments will be evaluated in BVS 611.

DRUG POSSIBLE REGIMEN COMMENTS

Dicloxacillin(Dynapen®) (Gen.) ۩

125-500mg PO q 6 hr AC Most adult doses range from 250-500mg. Renal dose adjustment needed.

Amoxicillin

(Amoxil®, others) (Gen.) ۩250mg – 1000mg PO T.I.D. Most adult doses range

from 250-500mg. Renal dose adjustment needed.

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BVS 611 – Pharmacology I

10. Anti-infective Medications

TYPICAL ADULT ORAL ANTI-INFECTIVE DOSES

DRUG POSSIBLE REGIMEN COMMENTS

Amoxicillin-clavulanate

(Augmentin®) (Gen.) ۩500/125: 1 tab PO T.I.D.

875/125: 1 tab PO B.I.D.

XR-1000/625: 2 tabs PO

B.I.D.

Need to clear both renal and hepatic status. Renal dose adjustment needed.

Ampicillin

(Principen®,others) (Gen.) ۩250mg-500mg PO q 6 hr Renal dose adjustment

needed.

Cefadroxil

(Duricef®) (Gen.) ۩500mg-1000mg PO q 12hr Renal dose adjustment

needed.

Cephalexin

(Keflex®) (Gen.) ۩250mg-500mg PO q 6hr Renal dose adjustment

needed.

Cefaclor

(Ceclor®) (Gen.) ۩250mg-500mg PO q 8hr Renal dose adjustment

needed.

Cefprozil

(Cefzil®) (Gen.) ۩250mg-500mg PO q 12hr Renal dose adjustment

needed.

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BVS 611 – Pharmacology I

10. Anti-infective MedicationsTYPICAL ADULT ORAL ANTI-INFECTIVE DOSES

DRUG POSSIBLE REGIMEN COMMENTS

Cefuroxime axetil (Zinacef®, Ceftin®) (Gen.) ۩

125mg-500mg PO q 12hr Most adult doses range from 250-500mg. Renal dose adjustment needed.

Cefdinir

(Omnicef®) (Gen.) ۩300mg PO q 12 hr

or

600mg PO q 24 hr

Renal dose adjustment needed.

Clindamycin

(Cleocin®) (Gen.) ۩150mg-450mg PO q6hr Hard to tolerate, high

potential for serious GI ADEs. Hepatic caution as well.

Azithromycin (Z-Pack®, Zithromax®, Zmax®)(Gen.) ۩ ****

Other strength products & preparations available.

For Z-Pack®: 2 x 500mg tabs PO on day 1, then 1 x 250mg tab PO on days 2-5.

Dose varies by indication. Hepatic drug clearance.

Erythromycin base and esters (Numerous products & preparations available; Eryc®, E-mycin®, EES®, etc.) (Gen.) ۩

250mg-500mg q 6 hr Dose varies by indication and product formulation. Can be hard to tolerate PO, hepatic and renal clearance.

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BVS 611 – Pharmacology I

10. Anti-infective Medications

TYPICAL ADULT ORAL ANTI-INFECTIVE DOSES

DRUG POSSIBLE REGIMEN COMMENTS

Clarithromycin

(Biaxin®) (Gen.) ۩500mg PO q 12hr Renal dose adjustment

needed, caution if hepatic problems as well

Doxycycline

Vibramycin®, Vibra-Tabs®, Doryx®, others) (Gen.) ۩

100mg PO q 12 hr Mostly hepatic clearance.

****

Tetracycline

(Sumycin®) (Gen.) ۩250-500mg PO q 6 hr Renal dose adjustment

needed.

Ciprofloxacin (Numerous products & preparations available.)

(Cipro®) (Gen.) ۩

500mg-750mg PO B.I.D. Renal dose adjustment needed.

Levofloxacin (Levaquin®) ۩ 250mg-750mg PO q 24hr Renal dose adjustment needed.

Moxifloxacin (Avelox®) ۩ 400mg PO q 24hr No renal adjustment needed. ****

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10. Anti-infective Medications

TYPICAL ADULT ORAL ANTI-INFECTIVE DOSES

DRUG POSSIBLE REGIMEN COMMENTS

Gemifloxacin

(Factive®)

320mg PO q 24 hr Renal dose adjustment needed. Very expensive, rarely prescribed for eye infections by O.D.s as less expensive, equally effective therapy is available.

Trimethoprim/sulfamethox-azole

(800mg SMX/160mg TMP = “double strength”)

(Bactrim DS®, Septra DS®) (Gen.) ۩

For CA-MRSA: 2 DS tablets PO B.I.D.

Renal dose adjustment needed. (Dose varies depending on whether double strength preparation is used.)

Acyclovir (Zovirax®) (Gen.) ۩

800mg PO 5x per day Renal dose adjustment needed. ****

Valacyclovir (Valtrex®) (Gen.) ۩

1000mg PO T.I.D. for VZV keratitis

Renal dose adjustment needed.

Famciclovir (Famvir®) ۩ 500mg PO T.I.D. Renal dose adjustment needed.

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10. Anti-infective Medications

Anti-infective Treatment Summary

BEFORE PRESCRIBING ANY ORAL MEDICATION, CHECK FOR BEFORE PRESCRIBING ANY ORAL MEDICATION, CHECK FOR POTENTIAL DRUG-TO-DRUG INTERACTIONS.POTENTIAL DRUG-TO-DRUG INTERACTIONS.

COMPARE THE DRUG THAT YOU ARE CONSIDERING COMPARE THE DRUG THAT YOU ARE CONSIDERING PRESCRIBING WITH THE OTHER MEDICATIONS ON THE PRESCRIBING WITH THE OTHER MEDICATIONS ON THE

PATIENT’S MEDICATION HISTORY/PROFILE.PATIENT’S MEDICATION HISTORY/PROFILE.

SEEK THE ASSISTANCE OF THE PATIENT’S PRIMARY SEEK THE ASSISTANCE OF THE PATIENT’S PRIMARY MEDICAL DOCTOR AND/OR A PHARMACIST IF NEEDED TO MEDICAL DOCTOR AND/OR A PHARMACIST IF NEEDED TO INTERPRET RELATIVE RISKS AND FOR OVERALL PATIENT INTERPRET RELATIVE RISKS AND FOR OVERALL PATIENT

SAFETY.SAFETY.

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BVS 611 – Pharmacology I

11. Antihypertensive Medications

Class Representative Drugs

Mechanism of Action

Uses Other Information

Centrally acting adrenergic nerve blockers

Clonidine (Catapres®), Guanabenz (Wytensin®), Guanfacine (Tenex®), Methyldopa (Aldomet®)

α2 agonists, decrease sympathetic outflow from brain to lower blood pressure

Hypertension Orthostatic hypotension, sedation and other ADEs possible. Blurred vision, conjunctivitis, and dry eyes are possible

Diuretics Several in different classes, see Diuretics section in syllabus

See Diuretics section in syllabus

Hypertension, edema, CHF

Thiazide diuretics currently used as initial medications for hypertension.

General Antihypertensive Classes

NOTE THAT THERE ARE MANY DIFFERENT CLASSES AS WELL AS INDIVIDUAL DRUGS USED FOR THE TREATMENT OF HYPERTENSION. STUDENTS SHOULD REFER TO THE DRUG INFORMATION

HANDBOOK FOR MORE DETAILS ON INDIVIDUAL AGENTS.

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11. Antihypertensive Medications

Class Representative Drugs

Mechanism of Action

Uses Other Information

Selective alpha-adrenergic antagonists

Prazosin (Minipress®), Doxazosin (Cardura®), Terazosin (Hytrin®), Tamsulosin (Flomax®)

Competitive blockade of alpha-receptors

Hypertension Doxazosin, Terazosin and Tamsulosin are also used for BPH

Orthostatic hypotension and other ADEs possible. Vision abnormalities (blurry vision, etc.) and conjunctivitis can occur. Intraoperative floppy iris syndrome possible in patients undergoing cataract surgery.

General Antihypertensive Classes

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11. Antihypertensive Medications

Class Representative Drugs

Mechanism of Action

Uses Other Information

Direct vasodilators

Hydralazine (Apresoline®), Minoxidil (Loniten®) Diazoxide (Hyperstat®), Nitroprusside (Nipride®)

Relaxes arterioles,

peripheral vasculature, and/or smooth muscles independent of sympathetic effects.

Hypertension and other specific uses.

Usually reserved for hypertensive crisis, accelerated hypertension, or advanced cases poorly controlled with more than one other class of antihypertensive agent. Hydralazine can cause lacrimation.

General Antihypertensive Classes

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11. Antihypertensive Medications

Class Representative Drugs

Mechanism of Action

Uses Other Information

Beta-adrenergic blocking agents

Labetalol (Trandate®), Carvedilol (Coreg®), Propranolol (Inderal®), Sotalol (Betapace®), Nadolol (Corgard®), MetoprololMetoprolol (Toprol XL®, Lopressor®), Timolol (Blocadren®, Timoptic®), Atenolol (Tenormin®) Acebutolol (Sectral®). Bisoprolol (Zebeta®), etc.

Competitive blockade of β-adrenergic receptors. Some agents are specific for β1 receptors at usual doses, while others have actions on both β1 and β2

receptors.

Hypertension. Some used also for cardiac arrhythmias, angina pectoris, glaucoma, migraine prophylaxis, MI prevention, CHF maintenance,etc.

Many potential ADRs and drug:drug interactions; individual agents need to be reviewed carefully when listed on a medication history. Use of these agents can cause dryness or soreness of the eyes, orthostatic hypotension, etc. Non-selective agents and high doses can exacerbate bronchospasm in asthma or COPD patients.

General Antihypertensive Classes

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BVS 611 – Pharmacology I

11. Antihypertensive Medications

Class Representative Drugs

Mechanism of Action

Uses Other Information

Calcium channel antagonists

Nifedipine (Procardia®), DiltiazemDiltiazem (Cardizem®), Verapamil (Calan®), Isradipine (Dynacirc®), Amlodipine Amlodipine (Norvasc®) and others

Blocks calcium influx during slow channel exchange, dilates peripheral arterioles, some are used for antiarrhythmic properties, also used for angina prophylaxis.

Angina prophylaxis, supraventri-cular tachycardia, hypertension

Many potential ADRs and drug:drug interactions; individual agents need to be reviewed carefully when listed on a medication history. Transient blindness has been reported rarely with nifedipine.

Aldosterone receptor antagonists

Spironolactone (Aldactone®), Eplerenone (Inspra®)

Blocks aldosterone binding to specific renal receptors

HypertensionCHF, CHF after after MI, edema

Can cause hyperkalemia and nephrotoxicity.

General Antihypertensive Classes

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BVS 611 – Pharmacology I

11. Antihypertensive Medications

Class Representative Drugs

Mechanism of Action

Uses Other Information

ACE-inhibitors

Captopril (Capoten®), LisinoprilLisinopril (Prinivil®, Zestril®), Enalapril (Vasotec®),Ramipril (Altace®), Quinapril (Accupril®) and others

Blocks conversion of angiotensin-I to angiotensin-II (a vasoconstrictor) and suppresses aldosterone, limiting sodium re-uptake in the kidney.

HypertensionCHF, MI

Can cause hypotension, dizziness, tachycardia, headache, cough, bradykinin accumulation. Many potential ADRs and drug:drug interactions; individual agents need to be reviewed carefully when listed on a medication history. Vision changes have rarely been reported.

General Antihypertensive Classes

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BVS 611 – Pharmacology I

11. Antihypertensive Medications

Class Representative Drugs

Mechanism of Action

Uses Other Information

Angiotensin receptor blockers (“ARBs”)

Losartan (Cozaar®), ValsartanValsartan (Diovan®), Irbesartan (Avapro®), Candesartan (Atacand®), Telmisartan (Micardis®) and others

Blocks angiotensin-II receptor site to control vasoconstriction. Also suppresses aldosterone.

Hypertension Hypotension, dizziness, and other ADEs possible. Conjunctivitis and blurred vision have been reported.

General Antihypertensive Classes

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BVS 611 – Pharmacology I

11. Antihypertensive Medications

TEACHING CASE: Patient with Hypertension

Clinical Clues:

Interventions:

Notes:

Recommendations:

A 56 year-old male patient is receiving his annual eye exam. On the medication history, the patient indicates that he takes hydrochlorothiazide 25mg PO once daily, and that his physician added metoprolol 50mg PO B.I.D. to his regimen three months ago. The only vision complaint that the patient reports since his last visit to the Optometry office is dry eyes.

The patient’s blood pressure in the office is 130/86.

Should the O.D. report this finding to the patient’s physician?Should the O.D. report this finding to the patient’s physician?

What is the pulse pressure differential based on this blood pressure reading? 4444

Can either of these medications cause or exacerbate dryness of the eyes?

Metoprolol, like all beta-adrenergic antagonists (or “beta blockers” can cause dry Metoprolol, like all beta-adrenergic antagonists (or “beta blockers” can cause dry eyes as an occasional side effect. The hydrochlorothiazide is a diuretic often used as eyes as an occasional side effect. The hydrochlorothiazide is a diuretic often used as first-line treatment of hypertension. Being a diuretic, it can theoretically first-line treatment of hypertension. Being a diuretic, it can theoretically

contribute to dry eyes if the patient becomes dehydrated.contribute to dry eyes if the patient becomes dehydrated.

Since the blood pressure appears to be coming under better control with the new regimen, the O.D. could recommend artificial tears to alleviate dryness of the eyes.

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This drug is prescribed for oral use by persons with Type 2 diabetes. It works by decreasing insulin resistance at peripheral sites and in the liver, but its best effect will result in a 0.5 – 1.4% reduction in hemoglobin A1c levels. The drug has also been associated with rare reports of causing decreased visual acuity and macular edema. This description best fits which of the following medications?

a.) metformin (Glucophage®)

b.) pioglitazone (Actos®)

c.) insulin aspart (Novolog®)

d.) pramlintide (Symlin®)

A 52 year-old male patient who is new to an optometrist’s practice reports that losartan (Cozaar®) is currently being taken. For which of the following conditions is this medication MOST likely prescribed?

a.) benign prostatic hyperplasia

b.) hyperthyroidism

c.) hypertension

d.) angina

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Which of the following dosage regimens would be APPROPRIATE when prescribing oral acyclovir (Zovirax®) in an adult patient with no known allergies?

a.) 250mg PO q 6 hr

b.) 400mg PO B.I.D.

c.) 500mg PO T.I.D.

d.) 800mg PO five times daily

This drug is approved for use in the treatment of supraventricular tachycardia, hypertension and angina. It blocks calcium influx during the slow channel exchange and dilates peripheral arterioles. The description of this drug most closely fits which of the following medications?

a.) nifedipine (Procardia®)

b.) lisinopril (Prinivil®)

c.) atenolol (Tenormin®)

d.) valsartan (Diovan®)

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BVS 611 – Pharmacology I

12. Diuretics

Diuretics treat edema and assist in blood pressure control by increasing urinary output. Diuretics specifically increase sodium and water excretion through the kidneys through a variety of mechanisms.

Thiazide Diuretics

Loop Diuretics

Potassium-Sparing

Diuretics

Carbonic Anhydrase Inhibitors

Osmotic Diuretics

Medication Examples

Hydrochloro-Hydrochloro-thiazide thiazide (“HCTZ”, Microzide®, (HydroDiuril®), Metolazone (Zaroxolyn®), Chlorthalidone (Thalitone®), etc.

FurosemideFurosemide (Lasix®), Bumetanide (Bumex®), Torsemide (Demadex®), Ethacrynic Acid (Edecrin®)

Spironolactone (Aldactone®), Amiloride (Midamor®), Triamterene (Dyrenium®)

Acetazolamide (Diamox®), Brinzolamide (Azopt®), Dorzolamide (Trusopt®)

Mannitol (Osmitrol®)

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BVS 611 – Pharmacology I

12. Diuretics

Diuretics treat edema and assist in blood pressure control by increasing urinary output. Diuretics specifically increase sodium and water excretion through the kidneys through a variety of mechanisms.

Thiazide Diuretics

Loop Diuretics Potassium-Sparing

Diuretics

Carbonic Anhydrase Inhibitors

Osmotic Diuretics

Uses Edema, hypertension

Edema, hypertension. Lasix also used for hypercalcemia

Edema, hypertension. Aldactone also used for cirrhotic ascites, CHF

Edema, acute mountain sickness, glaucoma

Acute glaucoma, diuresis, reduce intracranial pressure, reduce renal toxicity with some chemo drugs

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BVS 611 – Pharmacology I

12. Diuretics

Diuretics treat edema and assist in blood pressure control by increasing urinary output. Diuretics specifically increase sodium and water excretion through the kidneys through a variety of mechanisms.

Thiazide Diuretics

Loop Diuretics

Potassium-Sparing

Diuretics

Carbonic Anhydrase Inhibitors

Osmotic Diuretics

MOA Inhibits Na+ and Cl- reabsorption in distal renal tubule

Inhibits electrolyte reabsorption in ascending loop of Henle

PROMOTES Na+ excretion, spares K+. Aldactone antagonizes aldosterone

Inhibits carbonic anhydrase, lower IOP

Osmosis effects to inhibit Na+ and water reabsorption

ADRs Causes loss of Na+, Cl-, K+ and other electrolytes. Increases blood glucose, cholesterol and uric acid levels.

Electrolyte imbalance, increased blood glucose levels, ototoxicity, renal toxicity, volume changes, etc. Can cause blurred vision.

Hyperkalemia possible, Na+ or water depletion, etc.

Stomach upset, inducing metabolic acidosis, dehydration, etc. Transient myopia has been reported.

Headache, N/V, dehydration, dizziness, etc.

Can cause blurred vision.

Page 65: BVS 611 Slide Deck II. Which of the following insulin products is a short-acting insulin? a.) insulin aspart b.) insulin glargine c.) insulin detemir

BVS 611 – Pharmacology I

12. Diuretics

Diuretics treat edema and assist in blood pressure control by increasing urinary output. Diuretics specifically increase sodium and water excretion through the kidneys through a variety of mechanisms.

Thiazide Diuretics

Loop Diuretics

Potassium-Sparing

Diuretics

Carbonic Anhydrase Inhibitors

Osmotic Diuretics

Drug Interactions

Several possible, check as needed.

Several possible, check as needed.

Several possible, check as needed.

Several possible, check as needed.

Comments Caution in patients with diabetes, history of gout, hypercholest-erolemia.

Used in patients with low GFR. Can be used with other drugs in hypertensive crisis

With exception of aldactone, not highly effective when used alone.

Rarely used orally, most ophthalmic use is topical.

Administered parenterally.

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BVS 611 – Pharmacology I

Important notation for individuals taking medications for treatment of Important notation for individuals taking medications for treatment of hypertension:hypertension:

Taking frequent or routine doses of aspirin or non-steroidal anti-inflammatory agents (NSAIDs) can blunt (or lower) the effect of

antihypertensive medication therapy in individuals with high blood pressure.

This is because of:

- decreasing the levels or effects of ACE inhibitors, beta blockers, ARBs, hydralazine, and all diuretics

- dose-dependent decreases in prostaglandin synthesis caused by NSAIDs can reduce renal blood flow.

(O.T… O.F.)

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BVS 611 – Pharmacology I

13. Anticoagulant and Antiplatelet Medications

Heparin WarfarinWarfarin (Coumadin®)

Uses

Prevention and treatment of venous thrombosis, treatment of pulmonary embolism. Also used during renal dialysis and open heart surgery to prevent clotting during extracorporeal circulation.

Used for deep vein thrombosis, atrial fibrillation (to prevent strokes), pulmonary embolism. Used also in patients after heart valve replacement, and in some patients with rheumatic or ischemic heart disease.

Mechanism of Action

Inhibits clotting factors, larger doses inactivates thrombin and clotting factors to prevent conversion of fibrinogen to fibrin.

Interferes with synthesis of vitamin K-dependent clotting factors (Factors II, VII, IX, X). Antagonizes vitamin K.

Admin/PK

Usually administered IV or subcutaneously. Metabolized hepatically. Dosage is regulated and titrated based on PTT results.

Administered orally. High degree of serum protein binding, long T1/2 (approximately 35-37 hours.) Metabolized hepatically.

ADEsBleeding, thrombocytopenia, hematoma, injection site necrosis

Bleeding, necrosis, GI upset

Anticoagulants

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BVS 611 – Pharmacology I

13. Anticoagulant and Antiplatelet Medications

Heparin WarfarinWarfarin (Coumadin®)

Drug Interactions

Bleeding risk increased when used with aspirin, NSAIDs, other anticoagulants /thrombolytics, dipyridamole. Several antibiotics, antithyroid medications, and other medications can increase anticoagulant effects. Digoxin, doxycycline and other tetracyclines, and some antihistamines can decrease anticoagulant effects.

NSAIDs, aspirin, clopidogrel, several antibiotics, heparin, thrombolytic agents can increase bleeding risk. Effects are decreased by concomitant use of drugs such as rifampin which induce cytochrome P450. Increased or high intake of green, leafy vegetables (which are high in vitamin K) decrease medication effect. Check for potential interactions before prescribing!

Other Information

Effects reversed by use of protamine. May be preferred over low-molecular weight heparin products (see below) in patients with severely impaired renal function.

Effects reversed by use of vitamin K.

Anticoagulants