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Oxprenolol-non-selective beta blocker with some intrinsic sympathomimetic activity.

Oxprenolol is a non-selective beta blocker with some intrinsic sympathomimetic activity. It is used for the treatment of angina pectoris, abnormal heart rhythms and high blood pressure. More

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Description

Oxprenolol is a non-selective beta blocker with some intrinsic sympathomimetic activity. It is used for the treatment of angina pectoris, abnormal heart rhythms and high blood pressure.

Generic Name

Oxprenolol-non-selective beta blocker with some intrinsic sympathomimetic activity.

Chemical names

Coretal; Dl-Oxprenolol; Trasicor; Oxprenololum

Brand names

Trasicor

IUPAC name

1-[2-(prop-2-en-1-yloxy)phenoxy]-3-[(propan-2-yl)amino]propan-2-ol

Pharmacokinetics

Actions

Oxprenolol is a non-selective beta blocker with some intrinsic sympathomimetic activity, is a lipophilic beta blocker which passes the BBB (blood-brain barrier) easily than water soluble beta blockers. As such, it is associated with a higher incidence of CNS-related side effects than hydrophilic ligands such as atenolol, sotalol and nadolol.

Dosage/Dosage form

The recommended dose is 80-160 mg/day in 2-3 divided doses.

Therapeutic uses

Used in the treatment of hypertension, angina pectoris, arrhythmias, and anxiety.

Adverse effects/Side effects

CHF, heart block, severe bradycardia, bronchospasm, pulmonary oedema, postural hypotension, prolonged PR interval, sinus arrest, palpitation, chest pain, peripheral vascular disorders, hot flashes, syncope; vertigo, lightheadedness, headache, dizziness, nervousness, anxiety, irritability, depression, sleep disturbances, hallucinations, slurred speech; sedation, dry skin, rash, pruritus; impotence, decreased libido, wt gain, hypoglycaemia; GI disturbances; thrombocytopenia, leukopenia; elevated LFTs; paraesthesia, weakness; keratoconjunctivitis, dry and itching eyes, blurred vision; tinnitus; increased BUN; dyspnoea, wheezing; diaphoresis.

Interaction

  • Hypotension, cardiac arrhythmias and cardiac arrest may occur with IV diltiazem and verapamil.
  • Bradycardic and hypotensive effects may be enhanced by fentanyl.
  • Excessive reduction of sympathetic activity may occur with MAOIs, reserpine, guanethidine.
  • Effect may be enhanced by cimetidine.
  • Additive CNS depression may occur with opiate analgesics, antihistamines, ethanol, psychoactive drugs.
  • May enhance the vasoconstrictive effects of ergot alkaloids.
  • Effect may be reduced with indometacin (and possibly other NSAIDs).
  • May enhance effects of insulin and oral antidiabetics.
  • Hypertensive reactions may occur with sympathomimetics e.g. epinephrine.
  • Myocardial depression may be additive with inhalant anaesthetics.
  • Ephedra, yohimbe and ginseng may exacerbate hypertension.
  • May enhance negative inotropic and negative dromotropic effect of quinidine, amiodarone, disopyramide.

Contraindications

Bronchospasm or asthma; sinus bradycardia; 2nd and 3rd degree AV block; uncontrolled heart failure; sick sinus syndrome; right ventricular failure, allergic rhinitis, secondary to pulmonary hypertension; cardiogenic shock.

Storage

Store at 30°C (86°F).

Information

Molecular weight

265.348

Molecular formula

C15H23NO3

CAS number

6452-71-7

Precautions

  • Oxprenolol is a potent beta-blocker and should not be administered to asthmatics because it can cause irreversible airway failure and inflammation.
  • History of severe anaphylaxis to allergens; treatment of anaphylaxis (e.g. epinephrine) may be ineffective in patients on β-blockers.
  • Do not withdraw abruptly (particularly in patients with coronary artery disease).
  • Compensated heart failure, DM, severe hepatic impairment or inflammatory diseases, myasthenia gravis, peripheral vascular disease (including Raynaud's), untreated phaeochromocytoma, history of psychiatric illness.
  • Pregnancy and lactation.
  • May impair ability to drive or operate machinery.