MBBS Pharmacology.pdf

8/13/2019 MBBS Pharmacology.pdf

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LIPID LOWERING

Class Drugs Description MoA Uses Adverse P.kinetics

HMG-CoA reductase

Inhibitor

(statins)

AtorvastatinLong Acting

HMG-CoA Cholestrol

Hyper LDL

Atheroma rupture

LDL-Oxidation

Endothelial function

Headache

GI upset

Muscle tender

(CPK)

Take at bedtime

(HMG-CoAr )Rosuastatin

Simvastatin Short Acting

Fibrates

GemfibrosilFibrates + PPRALL

VLDL (TG)Hyper TG

Myalgia

Hepatitis

Gall Stones

G + Statin = myopathy

FenofibrateF/B + Statins = Safe

Bezafibrate

Nicotinic Acid Niacin + HDL

FFA Liver

formation of Hepatic VLDL

circulating TG

Hyper TG

Skin Flush, Heat

Dyspepsia,

Vomitting

Liver Toxicity

+ Statins = myopathy

Ezetimibe Inhibit cholesterol absorption Hyper LDLReversible Liver

ImpairedCombine with statins

Drugs LDL TGL HDL

Statins

Fibrates

Niacin

Ezetimibe

ANTI-ANGINAL


Organic Nitrate

Nitroglycerin Sublingual

Venodilate (Preload)

Artery Dilate (Afterload)

Unstable Angina

CHFAcute LVF

Acute MI

Cardiac Procedures

HeadacheReflex Tachycardia

Postural Hypotension

+ sidenafil - BP

Less FPMIsosorbide-Dinitrate

Isosorbide-5-mono

CCB

NifedipineDHP (VD)

HR, FC O2 demand

Artery Dilate TPR / afterload

Coronary flow

DVD: Angina, HTN

VD: SV arrhythmia

V: migraine prophylaxis

Constipation

Peripheral Edema

Hypotension

Reflex Tachycardia

(Worsen Angina)

Reflex Tachycardia:

Amlodipine

DHP + Beta-Blocker

Amlodipine

Verapamil VD, FC, HR

Diltiazem VD, FC, HR

HMG-CoAr

X


4/20

Beta-Blocker

AtenololB1-Selective

HR, FC O2 demand

Prophylaxis:

Myocardial Infarction

Angina

(more important in CHF)Metoprolol

PropanololB1 + B2

Timolol

Late Na Current Block Ranolazine Ca in Myocardium Angina Torsades de Pointes No effect on HR, BP

Anti-thrombotic

Low-Dose Aspirin

Prevent clotting Angina Bleeding Combination TherapyHeparin

Warfarin

ANTI-HYPERTENSIVE


1-blocker

Pra^zosin

Selective Block 1VD (BP)Hypertension

BPH

Ortho. Hypotension

Reflex Tachycardia

Nausea

Rhinitis

Urination

Tera^zosin

Doxa^zosin

Phenoxybenzamine Non-selective

Irreversible

Block 1 + 2 Pheochromocytoma

Phentolamine

2-agonist

ClonidineCentral Acting

+ Imidazoline

sympathetic activity (E, NE)

VD Artery

Hypertension

Menopause

Tiredness

Depression

Dry Mouth

CI: Renal FailureMethyl Dopa

Menoxidine

Beta-Blocker

Atenolol B1 Selective

1. HR, FC CO

2. X-B1 X-Renin X-AT2

3. Block 1 VD

4. Nebivolo +NO

Hypertension

Angina

Post-MI

CHF

Asthma (B2)

++ COPD

Bradycardia

Tiredness

CI: Asthma (B2)

ISA (Intrinsic

Sympathomimetic

Activity)

TimololB1 + B2

Propanolol

Nebivolol B1 + VD

Pindolol (ISA) B1 + B2 + VD

Carvedilol B1 + B2 + 1

Diuretics

Thiazides Na/Cl

Volume BPHypertension

Edema

Hypokalemia

CI: HyperuricaemiaAmiloride

Na BlockerHyperkalemiaTriamterene

Spironolactone X-Aldosterone


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RAAS

Alis^kiren Renin Inhibitors

*Refer RAAS Hypertension

Hypotension

Headache

Angioedema

Val^sartan

ARBIrbe^sartan

Telmi^sartan

Enala^pril ACE Inhibitors

VD

CCB DHP + Diltiazem

VD BP HypertensionMyocardial Ischemia

Peripheral Edam

Hyptension

Reflex Tachycardia

Hydralazine Artery Dilator

Na Nitroprusside Nitro VD

Congestive Heart Failure (CHF)


Preload

Frusemide Diuretics (X-Na-K-Cl) : PreloadCHF: Class 2, 3, 4

(+ symptoms)Hypomagnesemia

Diuretic Resistance:

Excess Na Intake

+NSAIDs

Renal Impaired

Enalapril

ACE Inhibitors X-AT2: VD, Aldosterone Hypertension

Hypotension

HeadacheDizziness

Ramipril

Lisinopril

Nitroglycerin Venodilators VD Preload CHF Hypotension Sublingual / IV

Afterload Hydralazine Artery Dilator Limit Ca Relax Smooth Muscle+ sympathetic reflex

(CI: angina + MI)

Oxidative Stress

Metoprolol

Beta-Blockers HR

CHF: 2,3 + HPT

Cardiac Remodelling

O2 demand

Asthma (B2)

Bradycardia

Paraesthesia

Worsen CHF (HR)Atenolol

Carvedilol

Contractility Digitoxin Glycosides

X-Na/K: FC SV

Peak Tension + Velocity

(Systole shorten Diastole prolong)

CHF + A.Fib

Notes

Toxicity Treatment

Notes:

Class I No Symptoms ACEI + BB AV Block Atropine

Class II S + Mid Exertion ACEI + D + BB + G Sinus Bradycardia Atropine

Class III S + Less Exertion ACEI + D + BB + G + VD SV Arrhythmia Propanolol

Class IV S at Rest All + IV D + IV VD + IV G V Arrhythmia Lignocaine


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BRONCHIAL ASTHMA


ACUTE TREATMENT

B2 Agonist Salbutamol Selective SABA +B2 : Bronchodilate First-line Asthma Tremor + Anxiety MDI (Inhale)

Leukotriene Inhibitor Theophylline X-Leukotrienes: Bronchoconstrict Asthma, COPD Arrhythmia, CNS + Found in Coco

Anti-cholinergic Ipratropium Br - Muscarinic : Bronchodilate Second-line Asthma Sedation, Dry Mouth MDI, Nebulizer

Adrenergic Agonist Epinephrine (E) cAMP : Bronchodilate Asthma, Allergy Tachycardia Oral

PROPHYLAXIS

GlucocorticoidBudesonide Anti-

InflammatorySuppress Immune : X mucus Chronic Asthma Super infection Oral, Parenteral

Beclomethasone

B2 AgonistFormoterol

Selective LABA +B2 : Bronchodilate Nocturnal Asthma Wheezing >12h + GlucocorticoidsSalmeterol

Leukotriene InhibitorZafirlukast

Anti-

Inflammatory

X-Leukotrienes: Bronchoconstrict Exercise-Induce Asthma Eosinophilia, Rash Oral, ChildrenMontelukast

Mast Cell Stabilizer Cromolyn Sodium X Histamine Release Allergic Dry Mouth MDI, DPI + LABA

COUGH


DemulcentsLozenges

+salivation +viscid layer sooth Symptomatic ReliefShort Acting

Effects Vanish w LayerSyrups

ExpectorantsPotassium Iodide SSKI Secretion

Productive Cough

Asthma

Gastric Irritant

Nausea

Require hydration

SSKI: Saturated Solution K I odideGuafenesin Secretion + Ciliary Action

Mucolytics Bromhexine Secretion + Ciliary Action Productive Cough Tears + Runny Nose Add in syrups

Antitussives

(suppress or relief cough)

Codeine

Opioid Suppress cough center selectively Unproductive coughConstipation

Respiratory DistressAdd with NSAIDs

Pholcodine

Noscapine

Non-Opiod Activate sigma receptor Unproductive cough Nausea + Vomitting

Dextropethorphan


7/20

Anti-Histamine

Diphenyhydramine1

stGeneration Block H1 receptor Allergic rhinitis Dizziness, Drowsy Cross BBB

Promethazine

Cetrizine (Zyrtec)2

ndGeneration Block H1 receptor Allergic rhinitis

Dry mouth

Blurred VisionNot cross BBB

Loratidine (Claritin)

Levocetirizine3

rdGeneration Block H1 receptor Allergic rhinitis Safer

Non drowsy

Rapid ActionFexofenadine

Decongestants Ephderine Sympathomimetic +Adrenergic VC Blood Nose blocked Insomnia, Anxiety CI: HypertensionPseudoephderine

HEMATINIC : + RBC


IRON

Ferrous SulphateDissociable

Ferrous Salt*not significant

Iron Def. Anemia

Epigastric pain

Nausea

Metallic Taste

Empty StomachFerrous Fumarate

Ferrous Gluconate

Iron DextranParenteral Iron Def. Anemia GI Upset

CI:Pregnant, Infants,

Children, GIT BleedIron Sucrose

B12

Cyanocobalamin

+ Intrinsic Factor Absorbed

Pernicious Anemia

Tapeworm

Ileectomy

Allergic CI: Folate Def. Anemia

Hydroxycobalamin PP Bound

Folate Increase folateMegaloblastic Anemia

Pregnancy (NTDs)Allergic CI: Pernicious Anemia

EPO Epoetin Alpha Recombinant + BM to produce RBCRenal Failure

Chemotherapy

Blood Viscosity

+ Clot

Flu-Like Symptoms

IV

IMMUNOSUPPRESSANT


Anti-proliferative

AzathioprineNon-Selective

+ 6-mercaptopurine

(Purine Analogue)

Inf. Bowel Disease

Rheumatoid Arthritis

BM Suppression

Liver ImpairCI: Allupurinol

Cyclophosphomide

Mycophenolate

mofetilIMP X Guanylyl (de novo) Prevent Graft Rejection GI ulceration, Edema

mTOR Inhibitor Sirolimus T-cell Activation Lymphoma Hypertension, Edema CI: Lung Transplant


8/20

Calcineurin InhibitorCyclosporine

Bind to Cyclophilin

X-NFAT : IL2 - T-cell DivisionGraft Rejection Hypertension CI: Renal Impaired

Tacrolimus

CorticosteroidsPrednisone

Steroid Supress IL2 Allergic, Autoimmune Weight Gain, Anxiety Slow Withdrawal

Dexamethasone

IL-2R Inhibitor

Basiliximab

Block IL2 Receptor Prevent Graft Rejection Opp. InfectionDaclizumab

ANTICOAGULANTS & THROMBOLYTICS


Fibrinolytic

Streptokinase Antigenic

Stroke

Acute MI

++ Pulmonary Embolism

Systemic Lytic

HemorrhageUrokinase Non-Antigenic

Alteplase Human tPA

Anticoagulant

Heparin

Unstable Angina

Bleeding, Osteoporosis Monitor aPTT

Enoxapain

LMW Heparin LessX-F10a Selectively

ThrombocytopeniaTinzaparin

Warfarin Oral

DVT

Pulmonary Embolism

Unstable Angina + MI

Bleeding

Teratogenic

High PP Bound

Start w Heparin (5 Days)

Antidote: Vit K

Anti-Platlet Drugs

LD Aspirin 75135 mgLD: X-TXA2

HD: X-PGI2 Prophylaxis: MI, Angina

Transient Ischemic Attack

Stroke

Coronary Angiplasty

Peri. Vascular Disease

GI Bleed

GI Irritation

Allergy

Thrombocytopenia

Clapidogrel

ADPr Inhibitor Bind to GP IIb/IIIa

Abciximab


9/20

PEPTIC DISEASE


H2-R Blocker

CimetidineDuodenal Ulcer

Gastric Ulcer

GERD

ZE Syndrome

Headache

Dizziness

Bowel Upset

Enzyme Inhibitor

Anti-Androgenic

RanitidineGood Oral

Antacids AbsorptionFamotidine

Nizatidine

PPI

OmeprazoleOral Duodenal Ulcer

Gastric Ulcer

GERD, ZE Syndrome

NSAIDs Induce Ulcer

Nausea

Headache

Abdominal Pain

Muscle Pain

+ Enteric Coated

(ionized at pH


10/20

5-HT3 BlockerOdan^setron

Anti-Emetic Block 5-HT3 Receptor (CTZ, GIT)Vomitting (X-Labyrinth)

Drug Induced Vomitting

Headache

Constipation5-HT3 = Serotonin

Grani^setron

M Blocker

Scopalamine

Anti Motion

Sickness

Block M Receptor (CTZ, Labyrinth)Prevent Motion Sickness

Otitis

Dry Mouth

Constipation

Blurred Vision

Transdermal Patch

Dicyclomine + with Ototoxic Drugs

(Aminoglycosides)Prochlorperaqzine

H1 BlockerPromethazine

Block H1 Receptor (CTZ, Labyrinth)Sedation

Psychomotor Control

+ D2 Blocker Toxicity

Diphenyhydramine

AdjuvantsDronabinol CB1R Agonist

*not significant Anti-Chemo VomittingPsycho Effect

SympathomimeticCorticosteroids Immunosupp.

GI MOTILITY


Laxatives

Fibre Diet Retain water Volume Functional Constipation - 2-3 days for effects

Docusate SodiumStool Softener

Stool Surface Tension Constipation

Liquid Paraffin Lubricates Hard Faeces Constipation 1-3 days

BisacodylPurgatives Secretions + Peristaltic

ConstipationAbdominal Cramp

Na Picosulfate Constipation

Mg SulfateSaline Laxative Retain water in lumen

Pre-Surgical CleansingFlatulence, Nausea

Lactulose Chronic Constipation Fructose + Lactose

Mosapride5-HT4 cAMP : Secretions

IBS, Chr ConstipationFlatulence

Non-ComplianceTegaserod

Enema Pro-kinetic + Bowel Distension : + Evacuation

Anti-Motility

ORS Rehydration Replace Fluid + Electrolyte Diarrhoea - Chronic : IV

Loperamide

Opiod

agonist : Activity

Non-Infective Diarrhoea

Abdominal Cramp

CI: ChildrenDiphenoxylate Cross BBB

Racecadotril X-Enkepalinase cAMP Nausea


11/20

DIABETES MELLITUS


Insulin Secretagogues

Glyburide

Sulfonylurea

Block S-R K Ca Influx

Normalization of FBS,

PPBG

HbA1c 1-2%

Hypoglycaemia

Weight Gain

Liver Failure

Renal Failure

: BB, NSAIDs

: Steroids

Take 30 min before meal

(Basal Insulin +)

Glipizide

Gliclazide

Glimepiride

Repoglinide

Meglitinide

Headache

Joint Pain

Weight Gain

Take 10 min before meal

( PP Insulin +)

HypoglycemiaNateglinide

Insulin Sensitizers

Metformin BiguanideSKM: Glucose Uptake

Liver: Gluconeogenesis

HbA1c 1-2%

Diarrhoea

Nausea

Abd Discomfort

Anorexia

Metal taste

Metformin : DOC

Take with Meals

No Weight Gain

CI: Renal Impaired

Pioglitazone

Thiazolidinedione

Activate PPAR-

SkM: Uptake, FA Flux,

Insulin Resistance

Liver: Gluconeogenesis

Rosiglitazone

Glucosidase Inhibitor

Acarbose

HbA1c 0.71.3%

Abdominal Discomfort

Flatulence

Bloating

Take with first bite

Miglitol

DPP-4 Inhibitor Sitagliptin

Inhibit DPP4 : Incretin Degrade

insulin secretions

Glucose Uptake

Hepatic Glucose Production

HbA1c 0.70.8Nasal Mucosa Inflamed

+ UTIIncretin: GLP-1, G1P

INSULIN


Rapid ActingLispro

3 -5 hoursPPBG Control

(Hypoglycaemia)

Subcutaneous

Dose = meal

515 min a/cAspart

Short Regular 68 hours Ketoacidosis (IV) 30 min a/c

IntermediateIsophane

2024 hoursSuspension

Lante X RegularLente


12/20

Slow

Ultra-Lente 36 hoursPh 5.4 (Dont Mix)

Determir 14 hours

Glargine 24 hours Peakless : Night Use

ANTI-THYROID


Anti-Thyroid

Propylthiouracil Inhibit Thyroid Peroxidase:X: Iodide tyrosyl

X: Iodide

X: Coupling (MIT, DIT)

X: Peri. Deiodination (T3 T4)

Prep Surgery

Control hypersecretion

Definitive Treatment

MaculopopularRash\Arthralgia

Agranulocytosis

Hypothyroid Baby

Less potent : q.i.dNot Cross Placenta

MethimazoleMore Potent : b.i.d

Cross Placenta

Ionic InhibitorThiocynates

Block Na/I Symporter Clinically Not UsedAplastic Anemia

Metallic Taste*Obselete

Perchlorates

Iodides ++ Iodide Thyroid Constipation Prep Surgery Edema + Swelling + Thioamide Agent

Radioactive Iodine

I127

Trapped in thyroid

+ with iodotyrosine Colloid

I123

- Thyroid Scan

*not fir for surgery

I131hypothyroidism

(follicular necrosis)CI : PregnancyI

131

I123

Scan

Beta - BlockerPropanolol

HRControl symptomsof

hyperthyroidsmAtenolol

ADRENOCORTICOSTEROIDS


Steroid CorticosteroidGlucocorticoid

Mineralocorticoid

Glucose:

Gluconeogenesis, UptakeAddisons Disease

Rheumatic Disease

Renal Disorders

Allergic Reaction

Bronchial Asthma

Infectious Disease

Ocular Disease

Skin Disease

GIT Disease

Chemotherapy

Skin: Delayed Healing

MSSK: osteoporosisCNS: Psychoses

Endocrine: Hypogonad

CVS: Hypertension

Immune: Opp. Infxn

GIT: Peptic Ulcer

Most: Oral

Dexamethasone: IM/IV

Insoluble: Intradermal

Local: Aerosol, Topical

Lipid:Fat Redistribution:

Buffalo Hump, Moon Face

Fluid & Electrolyte: Aldosterone

Skeletal Muscle:

Weakness, Myopathy, Ca

CNS: Mood, Psychosis

Stomach: ++ peptic ulcer

Anti-Inflammatory: Lipocortin


13/20

KIDNEY


Loop Diuretic

Frusemide

X-Na/K/Cl SympX:Na/K/ClThick Asc. Limb

(Block NaCl Reabsorption)

Pulmonary Edema

Cardio + Renal Edema

Forced Diuresis: Overdose

Fluid & Electrolyte Imb

Alkalosis

Ototoxicity

Hypomagnesemia

X-Sulfonylurea

X-NSAIDsTorasemide

Thiazides

Hydrochlorothiozde

X-Na/Cl Symp X-Na/ClDistal Conv. Tubule(Block NaCl Reabsorption)

Hypertension

Cardio + Renal EdemaKidney Stones

Fluid & Electrolyte Imb

UricaemiaSexual Dysfunction

Photosensitivity

X-NSAIDs ()

X-Digoxin ()

+K sparing (Amiloride)

Polythiazide

Indapamine

Chlorthalidone

K+ Sparing

Spironolactone

X-Aldosterone

Block Aldosterone Receptor

Late Distal Tubule + C.Duct

(Na, H20 + K secretions)

Hyperaldosterone (Conn)

Hypertension, Edema

Altered Sexual

CharacterCI: Hyperkalemia (K)

Eplerone

AmilorideX-ENaC

X-ENaCCollecting Duct

(Na, H20 Secretions)Hypertension, Edema

Hyperkalemia (K)

Photosensitivity

*ENaC: Epi Na Channel

+ Thiazides (K loss)Triamterene

Osmotic Diuresis Mannitol GFR (Prox. Conv Tubule) Cerebral Edema CI: Edema

CA InhibitorsAcetazolamide X-CA : X formation of H2CO3

(+ Metabolic Acidosis)

Secretions of Na, K, Cl, HCO3

Glaucoma

Altitude Sickness

Allergic

Bone Marrow Suppress

Not useful to mobilize

edemaDorzolamide

ORAL CONTRACEPTIVES


CombinedOestrogen

Gn Release X-FSH + LH Peak

X Ovulation

Modify F. Tubes contraction

Implantation of Blastocyst

Oral ContraceptivesThrombophlebitis

Thromboembolism

Hypertension

Cancer

Gall Stones

CI: Hypertension

X-antibiotics

X-Enzyme Inhibitors

Progesterone

Sequential Pill

Oestrogen 16 days

O + P 5 days

DF 7 daysMini Pill Progesterone Low Dose Less Effective

Post-CoitalMifepristone 72 hours

+ IUD after 5 daysNorgestrel 12 hours

Implant Norplant 6 Levonorgestrel

Contraceptives

Most Effective

Vaginal Hormone Nuvaring EE + Etonogastrel Flexible (Upper Vagina)

Transdermal Norgestimate EE + Norgestrmn


14/20

IUD

Copper

Progesterone

Levonorgestrel

PARKINSON


DA Precursor Levo-dopa DA in Basal Ganglia Parkinson

GI Upset

Ortho. Hypotension

CNS: confusion

+ Peri. Dopa-

Decarboxylase Inhibitor

(Carbidopa)

+Drug Holiday

DA-R AgonistPergolide

Ergot Alkaloids+DA Receptor at Corpus Striatum

(+ GP internal)Advance PD

Similar to L-Dopa

Retroperi. Fibrosis

Digital Vasospasm

Start w Low DoseBromocriptine

MAO-I Selegiline X-MAO-BSelective Irr. Inhibit MAO-B

DA Breakdown, DA EffectsEarly Mild PD Dry Mouth. Insomnia X-Cheese (Tyrosine)

Muscarinic Antagonist

Diphenyhydramine

ACh Block Ach ReceptorDrug-Induced PD

(metoclopromide)

Drowsiness

Confusion

Dry Mouth

Start w Low Dose

CI: BPH, Glaucoma

Benztropine

Bipiredin

COMT-ITolcapone

Adjuvant The amount of L-Dopa Cross BBB Adjunct: L-Dopa/Carbi HepatotoxicityEntacapone

Anti-Parkinsonism Amantidine Anti-Viral Alter uptake + release of DA Mild PD Lethargy, Insomnia Less Efficacious

SEDATIVES & HYPNOTICS


Benzodiazepines

(TLAD)

Triazolam Rapid-Acting

(


15/20

Non-Benzodiazepines

Zolpidem

Bind to GABA-A Receptor InsomniaHallucinations

AmnesiaCI: Driving, Elder, GERDZaleplon

Zopiclone

Atypical Anxiolytics Buspirone Serotonin 5HT1A Partial Agonist GAD:Gen Anxiety Disorder Dizziness, Nausea Less Sedation & Depndce

Beta-Blocker Propanolol X-Beta Adrenergic Receptor Performance-Induced

Misc.

Melatonin Reset Circadian, Jet Lag

Note:

Sedative : + calm

Hypnotics : + sleep

Promethazine Anti-histamine Surgical PrepOpiod

Amytriptyline SSRIs, TCA Anti-Depressant

OPIOD ANALGESICS


agonist

Morphine

Analgesic Pathway - Sensory

LimbicTranquillity, Euphoria

Locus Cerulus - Fear, Anxiety

Cough Center - Cough

Respiratory Center - Resp.

+ CTZ-VomitingEWN-Pupil Constriction (Pin-Point)

+Histamine : VD, Skin Itchy

Pain - COCardio-protective

GIT: Peristaltic, Secretions

Spasm of Sphincter of Oddi

Cancer Pain

Fracture Pain

Post-Op Pain

Biliary Colic

MI, LVF

Balanced Anesthesia

Visceral Pain (X-MSSK)

Nausea, Vomiting

Constipation

Biliary Tract Pressure

Urinary Retention

Hypotension, PruritusDrowsiness

Mental Clouding

Resp Depression

+ Tolerance

+ Dependence

+ Abuse

Precaution:

Pulmonary DiseaseHypotension, Shock(VD)

Head Injury

(ICP by CO2 Retention)

Neonate

Renal, Liver Impaired

CodeineMorphine

CongenersCough Center Dry Cough, MSSK Pain

Constipation

DrowsinessLess Analgesic Effects

Tramadol Serotonin, NE ReuptakeDepression

Fibromyalgia

Nausea, Vomiting

Constipation

+ Dependence

Better Oral Efficacy

Less Resp. Depression

Less Constipation

Pethidine Bind to , and also receptorObstetrics

(Labor Pain)

Resp. Depression

Tachycardia (IV)

Pupil Dilation

+ Dependence

Aka: Meperidine,Demerol

CI: MAO-I

Fentanyl Bind to receptor

Epidural: Post-Op, Labor

Transdermal: Cancer

IV: During Surgery

Hypoventilation100x Analgesic: Morphine

Rapid + Short Acting


16/20


17/20

Gametocidal

Primaquine Unknown

Radical Cure

Infection Control

Prevent Relapse

(Kill Hypnozoites)

Abdominal Pain

GI Upset

MetHbnemia +

cyanosis

CI: G6PD

Radical Cure

Others

Mefloquine

Clinical Cure

(+Artesunate)ACT Rationale:

Resistance to Chq Protect resistance declined efficacy More effective

P. falciparum:

20x merozoites Cerebral toxicty Bilirubin load Hypovolemia Chq Resistance

PYR+Sulfadoxine (+Artesunate)

Lumefantrine (+Artemether)

Doxycycline (+Quinine)

Proguanil Chemoprophy.

ANTI-TUBERCULOSIS


Anti-Tuberculosis

Isoniazid INH Inhibit Mycolic Acid (Cell Wall)

Bactericide:Rapid Multiply

Bacteristatic: Slow Grow

Intra & Extracellular

Hepatic Toxicity

PNS & CNS Toxicity

Urinary Retention

+ Resistance

Enzyme Inhibitor

I: Phenytoin

Rifampicin

X-DNA-Dependent RNA Polymerase

X RNA Transcription

Bactericide: All Subpop.(Except DormanT)

Intra & Extracellular

Resistance Prevention

Hepatitis

Flu-Like Syndrome

Orange Body Secretion

Enzyme Inducer

Pyrazinamide PZA

Pyrazinamidase convert PZA to

Pyrazinoic Acid (active form) ++

Disrupt Membrane Potential

Interfere with Energy +

Short-Term therapy for

Uncomplicated TB

Intracellular

Decrease Relapse Rate

Liver Damage

Hyperuricemia + Gout

Arthralgia

Rash + Fever

Bacteriostatic

Ethambutol EMB Inhibit Cell Wall SynthesisCombination Therapy

Suppress Growth Res. TBVisual Disturbance CI: Children (< 6 y/o)

Streptomycin Aminoglycoside Bind to 30SInterfere Proofread ExtracellularX-Vestibulocochlear (8)

NephrotoxicityIM Injection only


18/20

ANTIBIOTICS


PROTEINSYNTHESISINHIBITORS

Macrolides

Erythromycin

Bind to 50s

X-Translocation

Gram +ve

Resp. Tract Infxn

Drug of choice:

M. pneumonia

Chlamydia

Diphteria

Pertussis

H pylori

H influenzae

Salmonella

Toxoplasmosis

Alternative:

Tetanus

Strep Tonsillitis

Pharyngitis

Pneumonia

Prophylaxis:

Rheumatic Fever

Endocarditis

Skin Rash

Thrombophlebitis

GI Disturbance

Torsades-de-Pointes

X-Cross BBB

Phagocytosis

into Synovial

Eliminated in Bile

Enzyme Inhibitors

(AE of other drugs)

X-statins:

Rhabdomyolysis +

myopathy

X-OCS:

Loss Effectiveness

H pylori

(Clarithro + Amoxicillin)

Clarithromycin

Gramve

H. influenzae

H pylori

Pharyngitis

Resp. Tract Infxn

Skin Rash

Nausea + Vomitting

Jaundice

AAD

Azithromycin

Gonorrhoea

Thyphoid

Chlamydia

T gondii

Abdominal Pain

Nausea + Diarrhoea

Cholestatic Hepatitis

AAD

Ketolides TelithromycinBind to 50s

X-Translocation

S. pneumonia (Erythromycin Res)

H influenzae, B pertussis*same as Clarithro

10x affinity for 50s bind

than erythromycin

LincosamidesClindamycin Bind to 50s

X-Translocation

Gram +ve (MRSA), Anaerobic

Protozoa (Malaria)

Thrombocytopenia

Diarrhoea, RashTopical: Acne Treatment

Lincomycin

Streptogramins

Quinupristin 3Bind to 50s

Dalfopristin change

ribosome structure

+ Quinupristin bind

Gram +ve : MRSA, VRENausea

Myalgia + Arthralgia

*combination reduce

resistanceDalfopristin 7

Fusidic Acids Sodium Fusidate Narrow-SpectrumBind to 50s

X-Translocation

Gram +ve, C perfringens

Conjuctivitis + Skin Infection

Teratogenic

Jaundice

Bacteriostatic

+Statins: Rhabdomyolysis

Fluoroquinolones

Norfloxacin 1st

GenerationX-bDNA gyrase

X-Supercoiling

X-bDNA synthesis

Salmonella, Shigella

UTi, Enteric Fever, Enterocolitis

Res. Tuberculosis, Meningitis

Nausea + Vomiting

Allergic

CNS Effects

Arthropathy

Norfloxacin: Topical

Enzyme Inhibitors (AE)

CI: Pregnancy

Ciprofloxacin 2nd

Generation

Levofloxacin 3rd

Generation

Trovafloxacin 4th

Generation


19/20

PSI

Aminoglycosides

Streptomycin

Natural

Bind to 30s

Interfere

Proofreading

+Abnormal Protein

Bacteriocidal

(*depends on conc)

Resistant Tuberculosis

Ototoxicity

Renal Failure

+ INH / EMB / PZA

Neomycin Gut Sterilization Topical

Tobramycin Gramve (pseudomonas)

Kanamycin Research (isolate bacteria)

GentamicinSynthetic

MRSA, Enterococci +Vancomycin: MRSA

Amikacin Multidrug-Res. Gram -ve

CELLWALLSYNTHESISINHIBI

TORS

BETA-LACTAMS

Penicillins

Penicillin G Natural

+-lactam Ring

Bind to PBP

X-transpeptidase

Inhibit Petidoglycan

Synthesis on Bact.

Cell Wall

Chronic Disease

Meningitis, Pneumonia, Syphilis

Endocarditis (+Gentamycin)

Allergy

Opp. Infections

Diarrhoea

(with Amoxicillin)

Rare:

Hemolysis

Nephritis

Neurtoxicity

Most Potent

Acid Labile

(-lactamase sensitive)

Penicillin V Semi-Synthetic Oral Infections Acid Stable

Methicillin

Penicillinase Res.

Identify MRSA

Anti-staphylococcal(Skin + Soft Tissue)

Cloxacillin

Oxacillin

Ampicillin Extended

Spectrum

Bite Wound Infections (ie. Bedbugs)

Amoxicillin Sinusitus, URT Infections Less Diarrhoea

PiperacillinNosocomial Pneumonia

Anti-pseudomonas

Piperacillin:

Most Potent

+TazobactamCarbenicillin

Ticarcillin

Cephalosporin

Cephazolin1

stGeneration

Bacteriocidal

Bind to PBP

X-transpeptidase

Inhibit Petidoglycan

Synthesis on Bact.

Cell Wall

Klebsiella sp, Surgical ChemoprophylaxisAllergic

Hemolytic Anemia

Thrombocytopenia

Neutropenia

-Liver Function

Opp. Infection

(AAD)

Cephalexin

Cefoxitin2

ndGeneration Diverticulitis, Pneumonia (+CAP)

Cefaclor

Cefixime3rdGeneration Gonorrhoea Cross BBB

Ceftriaxone

Cefepime4

thGeneration Nosocomial Pneumonia (Pseudomonas)

Cefpirome

Monobactam Aztreonam Gramve, Penicillin allergic patients Nausea + Vomiting Non-Toxic

CarbapenemsImipenem Wide Range Gram +ve Gramve

(except Chlamydia)

Allergic

CNS Effects

Highly Resistance to

-lactamaseMeropenem


20/20

Beta-Lactamase

Inhibitors

Clavulanic AcidInactivate

Beta-Lactamase

Protect Antibiotics

(from destroyed by B-Lactamase)Combined with PenicillinSulbactam

Tazobactam

OthersVancomycin MRSA, Pseudomembranous Colitis

+Gentamycin

+Metronidazole

Bacitracin Strep. Pyogenes, Topical Antibiotics

BRO

AD-SPECTRUM

ChloramphenicolBind to50S

X-Transpeptidation

Bacterial Meningitis, Staph Brain Abscess

Enteric Fever

Intra-Abd Abscess (B fragillis):

+Metronidazole

Tetracycline Resistance:

Cholera, Rickettsia

GI Disturbance

Opp. Infection

Bone Marrow

Aplastic Anemia

Gray-Baby Syndrome

Cross Placental + BBB

Highly Toxic

Inactivated by Hepatic

Glucoronyltransferase

Bacteriostatic + cidal

Tetracycline

Tetracycline

Short Acting Bind to 30S

Inhibit the

attachment of tRNA

X-transcription

Rickettsia, Psittacosis, Chlamydia

Brucellosis, CholeraGI Disturbance

Super-Infection

Hepatic, Renal Toxicity

Photosensitivity

Vestibular Toxicity

Impaired by Food+

(Ca, Dairy, Iron, Al)

Cross Placenta

CI: Pregnancy

Chlortetracycline

OxytetracyclineDemoclocycline Intermediate Lyme, Acne, Bronchitis + SIADH

DoxycyclineLong Acting

Psittacosis, Syphilis, Chlamydia + Malaria

Chemoprophylaxis : AnthraxMinocycline

Co-trimoxazole

Trimethoprim 1Ind: Bacteristatic

Comb: Bactericide

HIV:prophylaxis for P. carinii

Bact:Travelers Diarrhoea, UTI

Protozoa: Isosporiasis, Toxoplasmosis

Nausea + Vomitting

Skin Rash

Stevens-Johnson

CI: PregnancySulfamethoxazol

e5

Documents

MBBS Pharmacology.pdf