Clinical Pharmacology Details


CAPTOPRIL


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Indications & Dose:

Adult


Hypertension,


initially 12.5 mg twice daily; if used in addition to diuretic, in elderly, or in renal impairment. Initially 6.25 mg twice daily (first dose at bedtime); usual maintenance dose 25 mg twice daily, max. 50 mg twice daily (rarely 3 times daily in severe hypertension).


Heart Failure:


(adjunct), initially 6.25 - 12.5 mg under close medical supervision; usual maintenance dose 25 mg 2-3 times daily, max; 150mg daily.. Diabetic


Nephropathy:


75-100mg daily in divided doses; if further blood pressure reduction required, other antihyper-tensive may be used in conjuction with captopril.


Severe renal impairment:


initially 12.5 mg twice daily (if concomitant diuretic therapy required loop diuretic rather than thiazide should be chosen).  


Prophylaxis:


After infraction in clinically stable patients with asymptomatic or symptomatic left ventricular dysfunction (radionuclide ventriculography or echocardiography undertaken before initiation). Initially 6.25 mg, starting as early as 3 days after infraction, then increased over several weeks to150 mg daily (if tolerated) in divided doses.


Diabetic nephropathy:


75-100mg daily in divided doses in divided doses; if further blood pressure reduction required other antihypertensive may be used


Child


Hypertension:


PO initial dose, 0.01 mg-0.25. mg/kg q 12h (infants); 0.0.5 mg tid (older children); maintenance dose, 2 mg/kg/dose bid-tid


Congestive heart failure


(left ventricular dysfunction): PO initial 2.5 mg/kg/ dose, increasing to 3.5 mg/ kg/dose, usually tid, with diuretics and digoxin

Contraindications:

Hypersensitivity to ACE inhibitors known or suspected renovascular disease,aortic stenosis or outflow tract obstruction,


pregnancy. Renal dysfunction, hypersensitivity.


 

Side Effects:

CNS: Chills, fever


CV: Chest pain, hypotension, palpitations, posturalhypotension, tachycardia


GI: Loss of taste


GU: Acute reversible renal failure, dysuria,frequency, impotence, nephrotic syndrome,nocturia, oliguria, polyuria, proteinuria


HEME: Agranulocytosis, neutropeni METAB: Hyperkalemia, hyponatremia


RESP: Angioedema, bronchospasm, cough,dyspnea


SKIN: Rash


 

Cautions:

Precautions:

History of anaphylaxis, renalinsufficiency (<30 ml/min), hypotension (CHF, elderly, volume depletion-diuretics, dialysis,cirrhosis), aortic stenosis, hyperkalemia (potassiumsupplements, potassium -sparing diuretics, renaldisease, diabetes), neutropenia (autoimmunediseases, collagen vascular, febrile illness,immunosuppressant drug therapy), proteinuria,renal artery stenosis, surgery/anesthesia (excessivehypotension, correctable with fluids).   


Breast- feeding & old age: May be used with caution.


 

Interaction:

Drugs


 Allopurinol: Increased risk of hypersensitivity reactions including Stevens-Johnson syndrome, skin eruptions, fever, and arthralgia


a-blockers: Possible exaggerated “first dose” response


Aspirin: Reduced hemodynamic effects of captopril; less likely at doses <236 mg qd


Azathioprine: Increased myelosuppression


Cyclosporine: Increased nephrotoxicity


Indomethacin: Inhibits the antihypertensive response to ACE inhibition; other NSAIDs probably have similar effect


Insulin: ACE inhibitors enhance insulin sensitivity; hypoglycemia possible


Iron: Increased risk of systemic reaction (GI symptoms, hypotension) with parenteral iron


Lithium: Increased risk of lithium toxicity


Loop diuretics: Initiation of ACE inhibition therapy with concurrent intensive diuretic therapy may cause significant hypotension, renal insufficiency


Mercaptopurine: Increased risk of neutropenia


Potassium, Potassium-sparing diuretics: ACE inhibition tends to increase potassium; increased risk of hyperkalemia in predisposed patients


Trimethtprim: Additive risk of hyperkalemia, especially  in  patient  predisposed  to  renal insufficiency


 


 

Warnings:

Adverse Effects:

Lactations:

Special Precautions:

Counselling:

Side Effects Or Adverse Reactions:

Patient And Carer Advice: