Pindolol

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Pindolol
Pindolol.svg
Pindolol3Dan.gif
Systematic (IUPAC) name
(RS)-1-(1H-indol-4-yloxy)-3-(isopropylamino)propan-2-ol
Clinical data
AHFS/Drugs.commonograph
MedlinePlusa684032
Pregnancy cat.C (AU) B (US)
Legal status Prescription only
Routesoral, iv
Pharmacokinetic data
Bioavailability50% to 95%
MetabolismHepatic
Half-life3–4 hours
ExcretionRenal
Identifiers
CAS number13523-86-9 YesY
ATC codeC07AA03
PubChemCID 4828
IUPHAR ligand91
DrugBankDB00960
ChemSpider4662 N
UNIIBJ4HF6IU1D N
KEGGD00513 YesY
ChEBICHEBI:8214 N
ChEMBLCHEMBL500 N
Chemical data
FormulaC14H20N2O2 
Mol. mass248.321 g/mol
 N (what is this?)  (verify)
 
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Pindolol
Pindolol.svg
Pindolol3Dan.gif
Systematic (IUPAC) name
(RS)-1-(1H-indol-4-yloxy)-3-(isopropylamino)propan-2-ol
Clinical data
AHFS/Drugs.commonograph
MedlinePlusa684032
Pregnancy cat.C (AU) B (US)
Legal status Prescription only
Routesoral, iv
Pharmacokinetic data
Bioavailability50% to 95%
MetabolismHepatic
Half-life3–4 hours
ExcretionRenal
Identifiers
CAS number13523-86-9 YesY
ATC codeC07AA03
PubChemCID 4828
IUPHAR ligand91
DrugBankDB00960
ChemSpider4662 N
UNIIBJ4HF6IU1D N
KEGGD00513 YesY
ChEBICHEBI:8214 N
ChEMBLCHEMBL500 N
Chemical data
FormulaC14H20N2O2 
Mol. mass248.321 g/mol
 N (what is this?)  (verify)

Pindolol (Visken, Betapindol, Blockin L, Blocklin L, Calvisken, Cardilate, Decreten, Durapindol, Glauco-Visken, Pectobloc, Pinbetol, Prindolol, Pynastin) is a beta blocker.

Pharmacology[edit]

Pindolol is a nonselective beta blocker with partial beta-adrenergic receptor agonist activity. It possesses ISA (Intrinsic Sympathomimetic Activity). This means that pindolol, particularly in high doses, exerts effects like epinephrine or isoprenaline (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 also functions as a 5-HT1A receptor weak partial agonist / antagonist (Ki=33nM[1]).

Pharmacokinetics[edit]

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 20 mg 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 pindolol is excreted in urine in unchanged form.

Indications[edit]

Investigational use[edit]

Contraindications[edit]

See also: Propranolol

Similar to propranolol with an extra contraindication for hyperthyroidism. In patients with thyrotoxicosis, possible deleterious effects from long-term use of pindolol have not been adequately appraised. Beta-blockade may mask the clinical signs of continuing hyperthyroidism or complications, and give a false impression of improvement. Therefore, abrupt withdrawal of pindolol may be followed by an exacerbation of the symptoms of hyperthyroidism, including thyroid storm.[4]

Pindolol has modest beta-adrenergic agonist activity and is therefore used with caution in angina pectoris.

Dosage[edit]

Usual doses are 5 mg 3 or 4 times daily or 15 to 20 mg in one single dose daily. Slow Release forms (20 mg) may be available to increase patient compliance. The maximum daily dose is 60 mg for hypertension and 40 mg 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 1 mg is injected i.v. under strict ECG-monitoring. Further treatment, if necessary, should then be oral.

The recommendation for augmentation in depressive patients is 2.5 mg (or possibly 5 mg) three times daily.

References[edit]

  1. ^ "PDSP". Retrieved 12 June 2013. 
  2. ^ Isaac MT (November 2004). "Review: combining pindolol with an SSRI improves early outcomes in people with depression". Evid Based Ment Health 7 (4): 107. doi:10.1136/ebmh.7.4.107. PMID 15504795. 
  3. ^ Safarinejad, MR (2008). "Once-daily high-dose pindolol for paroxetine-refractory premature ejaculation: a double-blind, placebo-controlled and randomized study.". Journal of Clinical Psychopharmacology 28 (1): 39–44. doi:10.1097/jcp.0b013e31816073a5. PMID 18204339. 
  4. ^ http://www.rxmed.com/b.main/b2.pharmaceutical/b2.1.monographs/CPS-%20Monographs/CPS-%20%28General%20Monographs-%20V%29/VISKEN.html