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PHARMACOLOGICAL COMPATIBILITY*

Propranolol Metabolization

Propranolol is a competitive antagonist drug of β1 and β2-adrenergic receptors, without intrinsic sympathomimetic activity.

CONTRAINDICATIONS

Hypersensitivity to propranolol or other β-blockers, cardiogenic shock, 2nd and 3rd degree atrioventricular block, uncontrolled heart failure, severe peripheral arterial circulation disorders, sick sinus syndrome, untreated pheochromocytoma, Prinzmetal angina, no ingestion after prolonged fasting, previous history of bronchial asthma or bronchospasm, patients with predisposition to hypoglycemia.

In addition, for solid forms it is contraindicated in the following cases: hypotension, metabolic acidosis, bradycardia. For liquid forms, it is also contraindicated in the following cases: premature infants, infants fed with breastfeeding if the mother is receiving drugs contraindicated with propranolol, bradycardia below the following limits:

0-3 months: heart rate 100 bpm; blood pressure 65/45 mmHg

3-6 months: heart rate 90 bpm; blood pressure 70/50 mmHg

6-12 months: heart rate 80 bpm; blood pressure 80/55 mmHg

CAUTIONS

1st degree heart blockade; diabetics; history of anaphylactic reactions, decompensated cirrhosis, hepatic insufficiency or significant renal insufficiency or in infants suffering from these pathologies.

Precautions should be taken in patients with portal hypertension, hepatic function may deteriorate and hepatic encephalopathy may develop. It can enhance muscle weakness in myasthenics, as well as mask signs of thyroxicosis.

In ischemic heart disease treatment should not be stopped abruptly.

Propranolol may mask the adrenergic warning signs of hypoglycaemia, as well as may aggravate hypoglycemia in children, especially in the case of fasting, vomiting or overdose.

In lower respiratory infection associated with dyspnea and wheezing, suspend treatment temporarily, and in case of isolated bronchospasm, suspend permanently.

In the case of surgery, beta-blockers produce an attenuation of reflex tachycardia and an increased risk of hypotension, and therefore it is advisable to discontinue treatment with beta-blockers at least 48 hours before the intervention.

SIDE EFFECTS

Fatigue, bradycardia, cold extremities, Raynaud’s phenomenon, sleep disorders and nightmares.

PHARMACOLOGIC INTERACTIONS

Propranolol potentiates the effect of insulin.

Potentiation of negative inotropic effects on heart when propranolol is ingested in concomitance with disopyramide and amiodarone.

Potentiation of toxicity with verapamil, diltiazem and bepridil.

Propranolol increases the risk of hypotension in concomitancy with nifedipine.

The effect of propranolol is antagonized by adrenaline.

Propranolol increases the plasma concentration of: lidocaine, possibly theophylline, warfarin, thioridazine and rizatriptan.

The plasma concentration of propranolol is increased by: cimetidine, alcohol, hydralazine; possibly by quinidine, propafenone, nicardipine, isradipine, nephodipine, nisoldipine and lacidipine.

Plasma concentration decreased possibly by rifampicin.

Propranolol increases the vasoconstrictive action of: ergotamine, dihydroergotamine or related compounds.

The hypotensive effect can be seen diminished by ibuprofen and indomethacin

BRAND NAME

  • Sumial ®

GENE OR REGION STUDIED


  • CYP2D6