This MedLibrary.org supplementary page on Pindolol is provided directly from the open source Wikipedia as a service to our readers. Please see the note below on authorship of this content, as well as the Wikipedia usage guidelines. To search for other content from our encyclopedia supplement, please use the form below:
Related Sponsors
 |
|
|
Pindolol
|
|
| Systematic (IUPAC) name | |
| 1-(1H-indol-4-yloxy)-3- (isopropylamino)propan-2-ol | |
| Identifiers | |
| CAS number | |
| ATC code | C07 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C14H20N2O2 |
| Mol. mass | 248.321 g/mol |
| Pharmacokinetic data | |
| Bioavailability | 50% to 95% |
| Metabolism | Hepatic |
| Half life | 3–4 hours |
| Excretion | Renal |
| Therapeutic considerations | |
| Pregnancy cat. | |
| Legal status |
℞ Prescription only |
| Routes | oral, iv |
Pindolol is a beta blocker drug.
Contents |
Pharmacology
Pindolol is a nonselective beta blocker in terms of cardioselectivity, but possesses ISA (Intrinsic Sympathomimetic Activity). This means that pindolol particularly in high doses exerts effects like epinephrine or isoproterenole (increased pulse rate, increased blood pressure, bronchodilation), but these effects are limited. Pindolol also shows membrane stabilizing effects like quinidine, possibly accounting for its antiarrhythmic effects. It acts on serotonin (5-HT1A) receptors in the brain resulting in increased postsynaptic serotonin concentrations.
Pharmacokinetics
Pindolol is rapidly and well absorbed from the GI tract. It undergoes some first-pass-metabolization leading to an oral bioavailability of 50 to 95%. Patients with uremia may have a reduced bioavailability. Food does not alter the bioavailability, but may increase the resorption. Following an oral single dose of 20mg peak plasma concentrations are reached within 1 to 2 hours. The effect of Pindolol on pulse rate (lowering) is evident after 3 hours. Despite the rather short halflife of 3 to 4 hours, hemodynamic effects persist for 24 hours after administration. Plasma halflives are increased to 3 - 11.5 hours in patients with renal impairment, to 7 - 15 hours in elderly patients, and from 2.5 to 30 hours in patients with liver cirrhosis. Approximately 2/3 of pindolol are metabolized in the liver giving hydroxylates, which are found in the urine as gluconurides and ethereal sulfates. The remaining 1/3 of pindolole is excreted in urine in unchanged form.
Uses
- Angina pectoris and hypertension. The use of pindolol in the treatment of unstable angina may be less effective compared to beta blockers without ISA.
- In some other countries also arrhythmias and prophylaxis of acute stress reactions.
Investigational use
- Augmentation therapy of clinical depression : Pindolol is sometimes added to a standard antidepressant therapy, if the patient fails to respond to the standard therapy alone. Fluoxetine is the most commonly used standard antidepressant. The results of augmentation therapy are encouraging. It is not known whether pindolol has antidepressive activities as monotherapeutic agent.
Contraindications and precautions
See the article on Propranolol.
Side effects
See the article on Propranolol.
Dosage
Usual doses are 5mg 3 or 4 times daily or 15 to 20mg in one single dose daily. Slow Release forms (20mg) may be available to increase patient compliance. The maximum daily dose is 60mg for hypertension and 40mg for angina. Treatment should be started with low doses and slowly increased according to the clinical response. The initial and maintenance doses should be reduced in patients with severe liver disease. In some countries pindolol exists as injection concentrate for the emergency treatment of serious arrhythmias. In these cases 0.4 to 1mg is injected i.v. under strict ECG-monitoring. Further treatment, if necessary, should then be oral. The recommendation for augmentation in depressive patients is 2.5mg (or possibly 5mg) three times daily.
Brand names
- Visken
- Betapindol
- Calvisken
- Decreten
- Durapindol
|
||||||||||||||||||||||||||||||
|
|||||||||||
External references
- AHFS Database
Wikipedia content modification information:
- This page was last modified on 24 July 2008, at 05:23.
Wikipedia Authorship and Review
Wikipedia content provided here is not reviewed directly by MedLibrary.org. Wikipedia content is authored by an open community of volunteers and is not produced by or in any way affiliated with MedLibrary.org.
Wikipedia Usage Guidelines
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article on "Pindolol".
The URL for this specific entry is:
All Wikipedia text is available under the terms of the GNU Free Documentation License. (See Copyrights for details). Wikipedia® is a registered trademark of the Wikimedia Foundation, Inc.