Wednesday, February 14, 2018

Dipyridamole-antianginal drug and its pharmacology.

DESCRIPTION:-

A phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. Dipyridamole also potentiates the antiaggregating action of prostacyclin.
This compound belongs to the class of organic compounds known as dialkylarylamines. These are aliphatic aromatic amines in which the amino group is linked to two aliphatic chains and one aromatic grouP.

PHRMACODYNAMICS:-

Dipyridamole, a non-nitrate coronary vasodilator that also inhibits platelet aggregation, is combined with other anticoagulant drugs, such as warfarin, to prevent thrombosis in patients with valvular or vascular disorders. Dipyridamole is also used in myocardial perfusion imaging, as an antiplatelet agent, and in combination with aspirin for stroke prophylaxis.

PHARMACOKINETICS:_

Absorption:- 70%
Volume of distribution :- 1 to 2.5 L/kg

Protein binding:- 99%
Metabolism:- hepatic
Route of elimination:- Dipyridamole is metabolized in the liver to the glucuronic acid conjugate and excreted with the bile.
Half life:-40 minutes
Clearance:-  2.3-3.5 mL/min/kg

Toxicity:-Hypotension, if it occurs, is likely to be of short duration, but a vasopressor drug may be used if necessary. The oral LD50 in rats is greater than 6,000 mg/kg while in the dogs, the oral LD50 is approximately 400 mg/kg. LD50=8.4g/kg (orally in rat)
Affected organisms:-  Humans and other mammals.

DRUG INTERACTION:-

1,10-Phenanthroline+dipyridamole =The therapeutic efficacy of 1,10-Phenanthroline can be decreased when used in combination with Dipyridamole.

Abciximab+ dipyridamole = Dipyridamole may increase the anticoagulant activities of Abciximab.

Acebutolol+ dipyridamole = Dipyridamole may increase the bradycardic activities of Acebutolol.

Acebutolol + dipyridamole:- The risk or severity of adverse effects can be increased when Acebutolol is combined with Dipyridamole.

Acenocoumarol+ dipyridamole = Dipyridamole may increase the anticoagulant activities of Acenocoumarol.

Acetaminophen + dipyridamole = The serum concentration of Acetaminophen can be increased when it is combined with Dipyridamole.

Acetazolamide + dipyridamole = The risk or severity of adverse effects can be increased when Acetazolamide is combined with Dipyridamole.

Acetylsalicylic acid+ dipyridamole = The risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Dipyridamole.

SIDE EFFECTS:-
less serious side effects:- dizziness;
    upset stomach, diarrhea, vomiting
    warmth, redness, or tingly feeling under your skin
    muscle or joint pain, headache
    mild skin rash or itching.

 serious side effects including: fainting, stomach pain, yellowing eyes/skin, dark urine, unusual bleeding/bruising...

THERAPEUTIC USES:-

This medication is used in combination with "blood thinners" such as warfarin to keep clots from forming after heart valve replacements. Clots are a serious complication that can cause strokes, heart attacks, or blocked blood vessels in the lungs (pulmonary embolisms). Dipyridamole is an antiplatelet drug. It helps to keep blood flowing by stopping platelets from clumping together and by keeping heart blood vessels open.

REFERENCE:-Tripathi K D"Essential of medical pharmacology",7th edition ,page no-553,629,630,633.

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