Blockin L: Full Drug Profile
Blockin L - General Information
A moderately lipophilic beta blocker (adrenergic beta-antagonists). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638)
Pharmacology of Blockin L
Blockin L is a non-selective beta-adrenergic antagonist (beta-blocker) which possesses intrinsic sympathomimetic activity (ISA) in therapeutic dosage ranges but does not possess quinidine-like membrane stabilizing activity. Blockin L impairs AV node conduction and decreases sinus rate and may also increase plasma triglycerides and decrease HDL-cholesterol levels. Blockin L is nonpolar and hydrophobic, with low to moderate lipid solubility. Blockin L has little to no intrinsic sympathomimetic activity and, unlike some other beta-adrenergic blocking agents, pindolol has little direct myocardial depressant activity and does not have an anesthetic-like membrane-stabilizing action.
Blockin L for patients
Patients, especially those with evidence of coronary artery insufficiency, should be warned against interruption or discontinuation of pindolol therapy without the physicianís advice. Although cardiac failure rarely occurs in properly selected patients, patients being treated with beta-adrenergic blocking agents should be advised to consult the physician at the first sign or symptom of impending failure.
Blockin L Interactions
Catecholamine-depleting drugs (e.g., reserpine) may have an additive effect when given with beta-blocking agents. Patients receiving pindolol plus a catecholamine-depleting agent should, therefore, be closely observed for evidence of hypotension and/or marked bradycardia which may produce vertigo, syncope, or postural hypotension.
Pindolol has been used with a variety of antihypertensive agents, including hydrochlorothiazide, hydralazine, and guanethidine without unexpected adverse interactions.
Pindolol has been shown to increase serum thioridazine levels when both drugs are co-administered. Pindolol levels may also be increased with this combination.
Risk of anaphylactic reaction: While taking beta blockers, patients with a history of severe anaphylactic reaction to a variety of allergens may be more reactive to repeated challenge, either accidental, diagnostic, or therapeutic. Such patients may be unresponsive to the usual doses of epinephrine used to treat allergic reactions.
Blockin L Contraindications
Pindolol tablets are contraindicated in:
1) bronchial asthma;
2) overt cardiac failure;
3) cardiogenic shock;
4) second and third degree heart block;
5) severe bradycardia.
Additional information about Blockin L
- Blockin L Indication
For the management of hypertension, edema, ventricular tachycardias, and atrial fibrillation.
- Mechanism Of Action
- Blockin L non-selectively blocks beta-1 adrenergic receptors mainly in the heart, inhibiting the effects of epinephrine and norepinephrine resulting in a decrease in heart rate and blood pressure. By binding beta-2 receptors in the juxtaglomerular apparatus, Blockin L inhibits the production of renin, thereby inhibiting angiotensin II and aldosterone production and therefore inhibits the vasoconstriction and water retention due to angiotensin II and aldosterone, respectively.
- Drug Interactions
- Acetohexamide The beta-blocker decreases the symptoms of hypoglycemia
- Generic Name
- Pindolol
- Drug Category
- Vasodilator Agents; Antihypertensive Agents; Adrenergic beta-Antagonists; Serotonin Antagonists
- Drug Type
- Small Molecule; Approved
- Other Brand Names containing Pindolol
- Betapindol; Blockin L; Blocklin L; Calvisken; Cardilate; Decreten; Durapindol; Glauco-Visken; Pectobloc; Pinbetol; Prinodolol; Pynastin; Visken;
- Absorption
- Rapidly and reproducibly absorbed (bioavailability greater than 95%).
- Toxicity (Overdose)
- LD50=263 mg/kg (orally in rats). Signs of overdose include excessive bradycardia, cardiac failure, hypotension, and bronchospasm.
- Protein Binding
- 40%
- Biotransformation
- Hepatic. In man, 35% to 40% is excreted unchanged in the urine and 60% to 65% is metabolized primarily to hydroxy-metabolites which are excreted as glucuronides and ethereal sulfates.
- Half Life
- 3 to 4 hours
- Dosage Forms of Blockin L
- Tablet Oral
- Chemical IUPAC Name
- 1-(1H-indol-4-yloxy)-3-(propan-2-ylamino)propan-2-ol
- Chemical Formula
- C14H20N2O2
- Pindolol on Wikipedia
- https://en.wikipedia.org/wiki/Pindolol
- Organisms Affected
- Humans and other mammals
