Drug literature

Feb . 17 201 1

DRUG STUDY

OXYTOCINGeneric Names:

Pitocin; Syntocinon Trade Names:

Oxytocin (BAM Biotech); Pitocin (Parke-Davis); Syntocinon (Sandoz)

Description

Synthetic 9 residue cyclic peptide. The hormone is prepared synthetically to avoid possible contamination with vasopressin (ADH) and other small polypeptides with biologic activity.

Indication

To assist in labor, elective labor induction, uterine contraction induction

ATC Therapeutic Category

H01BB:Oxytocin and analogues

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Binds the oxytocin receptor which leads to an increase in intracellular calcium levels.

Pharmacology

Used to induce labor or to enhance uterine contractions during labor. Uterine motility depends on the formation of the contractile protein actomyosin under the influence of the Ca2+-

dependent phosphorylating enzyme myosin light-chain kinase. Oxytocin promotes contractions by increasing the intracellular Ca2+, which in turn activates myosins light chain kinase.. Oxytocin has specific receptors in the muscle llining of the uterus and the receptor concentration increases greatly during pregnancy, reaching a maximum in early labor at term.

Absorption, Distribution, Metabolism, Elimination & Toxicity

Protein Binding-30%

Chemical Properties

Isomeric SMILES CC[C@H](C)[C@H]1C(=O)N[C@H](C(=O)N[C@H]

(C(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@H](C(=O)N1)CC2=CC=C(C=C2)O)N)C(=O)N3CCC[C@H]3C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N)CC(=O)N)CCC(=O)N

FUROSIMIDE

Generic Names: Dihydroflumethiazide; Frusemid; Frusemide;

Furosemid; Furosemida [INN-Spanish]; Furosemidu [Polish]; Furosemidum [INN-Latin]; Fursemid; Fursemida; Fursemide; Metflorylthiazidine; Methforylthiazidine

Trade Names: Aisemide; Aldalix; Aldic; Aluzine; Anfuramaide; Apo-

Frusemide; Apo-Furosemide; Aquarid; Aquasin; Arasemide; Beronald; Bioretic; Bristab; Bristurin; Cetasix; Depix; Desal; Desdemin; Di-Ademil; Dirine; Disal; Discoid; Disemide; Diucardin; Diumide-K;

Feb . 17 201 1

DRUG STUDYDiural; Diurapid; Diuretic Salt; Diurin; Diurolasa; Diusemide; Diusil; Diuzol; Dranex; Dryptal; Durafurid; Edemid; Edenol; Eliur; Elodrine; Endural; Errolon; Eutensin; Farsix; Finuret; Fluidrol; Fluss; Franyl; Frumex; Frumide; Frumil; Frusedan; Frusema; Frusemin; Frusenex; Frusetic; Frusid; Fulsix; Fuluvamide; Fuluvamine; Furanthril; Furanthryl; Furantril; Furanturil; Furesis; Furetic; Furex; Furfan; Furix; Furmid; Furo-Basan; Furo-Puren; Furobeta; Furocot; Furodiurol; Furodrix; Furomen; Furomex; Furomide M.D.; Furorese; Furosan; Furose; Furosedon; Furosemix; Furoside; Furosifar; Furosix; Furoter; Furovite; Fursol; Fusid; Golan; Hissuflux; Hydol; Hydrenox; Hydrex; Hydro; Hydro-Rapid; Hydroled; Impugan; Jenafusid; Katlex; Kofuzon; Kolkin; Kutrix; Lasemid; Lasex; Lasiletten; Lasilix; Lasix; Lasix Retard; Lasix Special; Laxur; Lazix; Leodrine; Less Diur; Liside; Logirene; Lowpston; Lowpstron; Luscek; Macasirool; Marsemide; Mirfat; Mita; Moilarorin; Myrosemide; Nadis; Nelsix.

Description A benzoic-sulfonamide-furan. It is a diuretic with fast

onset and short duration that is used for edema and chronic renal insufficiency.

Indication For the treatment of edema associated with

congestive heart failure, cirrhosis of the liver, and renal disease, including the nephrotic syndrome. Also for the treatment of hypertension alone or in combination with other antihypertensive agents.

ATC Therapeutic Category C03CA:Sulfonamides, plain

Pharmacology, Interactions, and ContraindicationsMechanism of Action

Furosemide, by inhibiting the reabsorption of sodium and chloride in the ascending limb of the loop of Henle, increases the urinary excretion of sodium, chloride, and water. Furosemide also increases the excretion of potassium, hydrogen, calcium,

magnesium, ammonium, and phosphate and, as it inhibits carbonic anhydrase, bicarbonate.

Pharmacology Furosemide, a sulfonamide-type loop diuretic

structurally related to bumetanide, is used to manage hypertension and edema associated with congestive heart failure, cirrhosis, and renal disease, including the nephrotic syndrome.

Food Interaction Avoid alcohol. Avoid excess salt/sodium unless otherwise instructed

by your physician. Increase potassium intake; add a banana or orange

juice; unless instructed otherwise. Take with food to reduce irritation.

Absorption, Distribution, Metabolism, Elimination & ToxicityProtein Binding- 99%Chemical PropertiesIsomeric SMILES

c1cc(oc1)CNc2cc(c(cc2C(=O)O)S(=O)(=O)N)Cl

DIPHENHYDRAMINE HCL

Generic Names: Diphenhydramine Base; Diphenhydramine Hcl;

Diphenhydramine Salicylate; Diphenylhydramine Trade Names:

Aleryl; Alledryl; Aller-Med; Allerdryl; Allergan B; Allergeval; Allergical; Allergin; Allergina; Allergival; Allermax Caplets; Ambodryl; Amidryl; Antistominum; Antitussive; Antomin; Automin; Bagodryl; Banophen; Banophen Caplets; Baramine; Beldin; Belix; Ben-Allergin; Bena; Benachlor; Benadrin; Benadryl; Benadryl Allergy; Benadryl Preservative Free; Benapon; Benodin; Benodine; Benylan; Benylin; Benzantine; Benzhydramine; Benzhydraminum; Benzhydril; Benzhydroamina; Benzhydryl; Betramin;

Feb . 17 201 1

DRUG STUDYCompoz; Dabylen; Debendrin; Dermistina; Dermodrin; Desentol; Diabenyl; Diabylen; Dibendrin; Dibenil; Dibondrin; Difedryl; Difenhydramin; Difenidramina; Dihidral; Dimedrol; Dimedryl; Diphantine; Diphen; Diphen Cough; Diphenhist; Diphenhist Captabs; Dormarex 2; Dryistan; Drylistan; Dylamon; Etanautine; Genahist; Histaxin; Hyadrine; Hydramine; Hyrexin; Ibiodral; Medidryl; Mephadryl; Nausen; Nervine Nighttime Sleep-Aid; Novamina; Nytol Quickcaps; Nytol Quickgels; Probedryl; Restamin; Rigidil; Rigidyl; Siladryl; Silphen; Sleep-Eze D; Sleep-Eze D Extra Strength; Sominex; Soverin; Syntedril; Syntodril; Torinal; Twilite Caplets; Unisom Sleepgels Maximum Strength; Vena; Vicks Formula 44

Brand Mixtures: Ambenyl Cough Syrup (Ammonium Chloride +

Bromodiphenhydramine Hydrochloride + Codeine Phosphate + Diphenhydramine Hydrochloride + Potassium Guaiacol Sulphonate); Benadryl Decongestant Tablets (Diphenhydramine Hydrochloride + Pseudoephedrine Hydrochloride); Bye Bye Bite Lot (Benzocaine + Diphenhydramine Hydrochloride + Menthol); Caladryl Cream (Calamine + Diphenhydramine Hydrochloride); Caladryl Lotion (Calamine + Diphenhydramine Hydrochloride); Calamine Lotion W Antihistamine (Calamine + Diphenhydramine Hydrochloride)

Description

A histamine H1 antagonist used as an antiemetic, antitussive, for dermatoses and pruritus, for hypersensitivity reactions, as a hypnotic, an antiparkinson, and as an ingredient in common cold preparations. It has some undesired antimuscarinic and sedative effects.

Indication

For the treatment of symptoms associated with Vertigo/Meniere's disease, nausea and vomiting, motion sickness and insect bite.

ATC Therapeutic Categories

D04AA:Antihistamines for topical use R06AA:Aminoalkyl ethers


Mechanism of Action

Diphenhydramine competes with free histamine for binding at HA-receptor sites. This antagonizes the effects of histamine on HA-receptors, leading to a reduction of the negative symptoms brought on by histamine HA-receptor binding.

Pharmacology

Diphenhydramine is an antihistamine of the ethanolamine class. Ethanolamine antihistamines have significant antimuscarinic activity and produce marked sedation in most patients. In addition to the usual allergic symptoms, the drug also treats irritant cough and nausea, vomiting, and vertigo associated with motion sickness. It also is used commonly to treat drug-induced extrapyramidal symptoms as well as to treat mild cases of Parkinson's disease. Rather than preventing the release of histamine, as do cromolyn and nedocromil, diphenhydramine competes with free histamine for binding at HA-receptor sites. Diphenhydramine competitively antagonizes the effects of histamine on HA-receptors in the GI tract, uterus, large blood vessels, and

Feb . 17 201 1

DRUG STUDYbronchial muscle. Ethanolamine derivatives have greater anticholinergic activity than do other antihistamines, which probably accounts for the antidyskinetic action of diphenhydramine. This anticholinergic action appears to be due to a central antimuscarinic effect, which also may be responsible for its antiemetic effects, although the exact mechanism is unknown.

Food Interaction

Avoid alcohol. Take with food


Biotransformation

Hepatic and renal

Protein Binding

98 to 99%

Absorption

Quickly absorbed with maximum activity occurring in approximately one hour.

Toxicity

LD 50=500 mg/kg (orally in rats). Considerable overdosage can lead to myocardial infarction (heart attack), serious ventricular dysrhythmias, coma and death.

Chemical Properties

Isomeric SMILES CN(C)CCOC(c1ccccc1)c2ccccc2

VASOPRESSIN

Generic Names: 3-Isoleucyl vasopressin; Arginine oxytocin; Arginine

vasotocin; Argiprestocin; Pitressin tannate; Vasopressin, isoleucyl; Vasopressin, non-mammalian; Vasotocin

Trade Names: Pitressin; Pressyn

Description

Antidiuretic hormone, also known as vasopressin, is a nine amino acid peptide secreted from the posterior pituitary. Antidiuretic hormone binds to receptors in the distal or collecting tubules of the kidney and promotes reabsorbtion of water back into the circulation

Indication

For the treatment of enuresis, polyuria, diabetes insipidus, polydipsia and oesophageal varices with bleeding

ATC Therapeutic Category

H01BA:Vasopressin and analogues


Feb . 17 201 1

DRUG STUDYMechanism of Action

Vasopressin acts on three different receptors, vasopressin receptor V1a (which initiates vasoconstriction, liver gluconeogenesis, platelet aggregation and release of factor VIII), vasopressin receptor V1b (which mediates corticotrophin secretion from the pituitary) and vasopressin receptor V2 which controls free water reabsorption in the renal medullar. The binding of vasopressin to the V2 receptor activates adenylate cyclase which causes the release of aquaporin 2 channels into the cells lining the renal medullar duct. This allows water to be reabsorbed down an osmotic gradient so the urine is more concentrated.

Pharmacology

Vasopressin is an antidiuretic hormone indicated for the prevention and treatment of postoperative abdominal distention, in abdominal roentgenography to dispel interfering gas shadows, and in diabetes insipidus. Vasopressin can cause contraction of smooth muscle of the gastrointestinal tract and of all parts of the vascular bed, especially the capillaries, small arterioles and venules. It has less effect on the smooth musculature of the large veins. Vasopressin may also be used to control bleeding in some forms of von Willebrand disease and to treat extreme cases of bed wetting in children. It may also play a role in memory formation although the mechanism is unknown.


Biotransformation

The majority of a dose of vasopressin is metabolized and rapidly destroyed in the liver and kidneys.

Protein Binding

1%

Chemical Properties

Isomeric SMILES

CC[C@@H]([C@H]1NC(=O)[C@H](NC(=O)[C@H](CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N2[C@H](CCC2)C(=O)N[C@@H](C(=O)NCC(=O)N)CCC/N=C(\N)/N)N)CC3=CC=C(C=C3)O)C

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