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{{Sotalol}}
{{drugbox |
| IUPAC_name = ''N''-[4-(1-hydroxy-2-isopropylamino-<br>ethyl)-phenyl]-methanesulfonamide
| image = Sotalol.png
| CAS_number = 3930-20-9
| ATC_prefix=C07
| ATC_suffix=AA07
| PubChem=5253
| DrugBank=
| C=12 | H=20 | N=2 | O=3 | S=1
| molecular_weight =  272.3624 g/mol
| bioavailability = >95%
| metabolism = Not metabolised
| elimination_half-life = 12 hours
| excretion = [[Kidney|Renal]] <br> [[Mammary gland|Lactic]] (In lactating females)
| pregnancy_AU =
| pregnancy_US = B
| pregnancy_category =
| legal_status = Rx-only
| routes_of_administration = oral
}}
__NOTOC__
__NOTOC__
{{Pindolol}}
{{CMG}}
{{CMG}}


'''''For patient information about Pindolol, click [[Pindolol (patient information)|here]].'''''
'''''For patient information about Sotalol, click [[Sotalol (patient information)|here]].'''''


{{SB}} Visken
{{SB}} BETAPACE, SOTALOL HYDROCHLORIDE


==Overview==
==Overview==


'''Pindolol''' ('''Visken''', '''Betapindol''', '''Blockin L''', '''Blocklin L''', '''Calvisken''', '''Cardilate''', '''Decreten''', '''Durapindol''', '''Glauco-Visken''', '''Pectobloc''', '''Pinbetol''', '''Prindolol''', '''Pynastin''') is a [[beta blocker]].
'''Sotalol''' (trade names '''Betapace''' and '''Betapace AF''', [[Berlex Laboratories]]) is a [[medication|drug]] used in individuals with rhythm disturbances ([[cardiac arrhythmia]]s) of the [[heart]], and to treat [[hypertension]] in some individuals.


==Category==
==Category==


Beta blockers
Beta Blockers


==FDA Package Insert==
==FDA Package Insert==


====Visken (pindolol) Tablet====
====BETAPACE (sotalol hydrochloride) tablet====


'''  [[Pindolol indications and usage|Indications and Usage]]'''
'''  [[Sotalol tablet indications and usage|Indications and Usage]]'''
'''| [[Pindolol dosage and administration|Dosage and Administration]]'''
'''| [[Sotalol tablet dosage and administration|Dosage and Administration]]'''
'''| [[Pindolol contraindications|Contraindications]]'''
'''| [[Sotalol tablet contraindications|Contraindications]]'''
'''| [[Pindolol warnings and precautions|Warnings and Precautions]]'''
'''| [[Sotalol tablet warnings and precautions|Warnings and Precautions]]'''
'''| [[Pindolol adverse reactions|Adverse Reactions]]'''
'''| [[Sotalol tablet adverse reactions|Adverse Reactions]]'''
'''| [[Pindolol drug interactions|Drug Interactions]]'''
'''| [[Sotalol tablet drug interactions|Drug Interactions]]'''
'''| [[Pindolol use in specific populations|Use in Specific Populations]]'''
'''| [[Sotalol tablet use in specific populations|Use in Specific Populations]]'''
'''| [[Pindolol overdosage|Overdosage]]'''
'''| [[Sotalol tablet overdosage|Overdosage]]'''
'''| [[Pindolol description|Description]]'''
'''| [[Sotalol tablet description|Description]]'''
'''| [[Pindolol clinical pharmacology|Clinical Pharmacology]]'''
'''| [[Sotalol tablet clinical pharmacology|Clinical Pharmacology]]'''
'''| [[Pindolol how supplied storage and handling|How Supplied/Storage and Handling]]'''
'''| [[Sotalol tablet clinical studies|Clinical Studies]]'''
'''| [[Pindolol patient counseling information|Patient Counseling Information]]'''
'''| [[Sotalol tablet how supplied storage and handling|How Supplied/Storage and Handling]]'''
'''| [[Sotalol tablet labels and packages|Labels and Packages]]'''


==Mechanism of Action==
{|
| [[File:Sotabb1.png|thumb|800px]]
|}


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|5-HT<sub>1A</sub> receptor]] weak [[partial agonist]] / [[receptor antagonist|antagonist]] (K<sub>i</sub>=33nM<ref>{{cite web|title=PDSP|url=http://pdsp.med.unc.edu/pdsp.php?|accessdate=12 June 2013}}</ref>).
====SOTALOL HYDROCHLORIDE injection====


==Pharmacokinetics==
'''  [[Sotalol injection indications and usage|Indications and Usage]]'''
'''| [[Sotalol injection dosage and administration|Dosage and Administration]]'''
'''| [[Sotalol injection dosage forms and strengths|Dosage Forms and Strengths]]'''
'''| [[Sotalol injection contraindications|Contraindications]]'''
'''| [[Sotalol injection warnings and precautions|Warnings and Precautions]]'''
'''| [[Sotalol injection adverse reactions|Adverse Reactions]]'''
'''| [[Sotalol injection drug interactions|Drug Interactions]]'''
'''| [[Sotalol injection use in specific populations|Use in Specific Populations]]'''
'''| [[Sotalol injection overdosage|Overdosage]]'''
'''| [[Sotalol injection description|Description]]'''
'''| [[Sotalol injection clinical pharmacology|Clinical Pharmacology]]'''
'''| [[Sotalol injection nonclinical toxicology|Nonclinical Toxicology]]'''
'''| [[Sotalol injection clinical studies|Clinical Studies]]'''
'''| [[Sotalol injection how supplied storage and handling|How Supplied/Storage and Handling]]'''
'''| [[Sotalol injection patient counseling information|Patient Counseling Information]]'''
'''| [[Sotalol injection labels and packages|Labels and Packages]]'''


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&nbsp;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.
{|
| [[File:Sotabb2.png|thumb|800px]]
|}


==Indications==
==Pharmacology==


* [[Angina pectoris]] and [[hypertension]]. The use of pindolol in the treatment of unstable angina may be less effective compared to beta blockers without ISA.
It falls into the class III [[antiarrhythmic agents]] because it inhibits the inward [[potassium]] [[ion channel]]s in the heart. It is also a [[beta blocker]] because of its primary action on the &beta;-[[adrenergic receptor]]s in the heart.
* In some other countries also [[arrhythmias]] and prophylaxis of acute [[Stress (medicine)|stress]] reactions.


==Investigational Use==
By blocking the [[potassium channel]]s, sotalol prolongs [[repolarization]], therefore lengthening the [[QT interval]] and decreasing [[automaticity]].


* Augmentation therapy of [[clinical depression]]: Pindolol is sometimes added to a standard antidepressant therapy,<ref name="pmid15504795">{{cite journal |author=Isaac MT |title=Review: combining pindolol with an SSRI improves early outcomes in people with depression |journal=Evid Based Ment Health |volume=7 |issue=4 |pages=107 |date=November 2004 |pmid=15504795 |doi= 10.1136/ebmh.7.4.107|url=http://ebmh.bmj.com/cgi/pmidlookup?view=long&pmid=15504795}}</ref> 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.
It also slows [[AV node|atrioventricular (AV) nodal]] conduction (beta-blocking effect).


* Augmentation therapy of [[premature ejaculation]]: According to a recent study, pindolol can be effectively added to a standard anti-premature-ejaculation therapy, which usually consists of daily doses of an SSRI antidepressant such as fluoxetine or paroxetine. Augmentation of pindolol results in substantial increase of ejaculatory latency, even in those who previously did not experience in an improvement with the SSRI monotherapy.<ref>{{cite journal | last1 = Safarinejad | first1 = MR | title = Once-daily high-dose pindolol for paroxetine-refractory premature ejaculation: a double-blind, placebo-controlled and randomized study. | journal = Journal of Clinical Psychopharmacology | volume = 28 | issue = 1 | pages = 39–44 | year = 2008 | pmid = 18204339 | doi = 10.1097/jcp.0b013e31816073a5}}</ref>
Sotalol is a [[racemic]] mix of D and L [[enantiomers]]. The ''L''-isomer is a [[beta blocker]].


==Contraindications==
Sotalol is not selected for its beta-blocking ability, but rather for its Class III (potassium blocking) properties.


{{See Also|Propranolol}}
==Indications==


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.<ref>http://www.rxmed.com/b.main/b2.pharmaceutical/b2.1.monographs/CPS-%20Monographs/CPS-%20%28General%20Monographs-%20V%29/VISKEN.html</ref>
Sotalol is used to treat [[ventricular tachycardia]]s as well as [[atrial fibrillation]]. Betapace AF is specifically labeled for [[atrial fibrillation]].


Pindolol has modest [[beta-adrenergic agonist]] activity and is therefore used with caution in [[angina pectoris]].
Some evidence suggests that sotalol should be avoided in the setting of decreased [[ejection fraction]] due to [[myocardial infarction|heart attack]].


==Dosage==
==References==


Usual doses are 5&nbsp;mg 3 or 4 times daily or 15 to 20&nbsp;mg in one single dose daily. Slow Release forms (20&nbsp;mg) may be available to increase patient compliance. The maximum daily dose is 60&nbsp;mg for hypertension and 40&nbsp;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&nbsp;mg is injected i.v. under strict ECG-monitoring. Further treatment, if necessary, should then be oral.
{{Reflist|2}}


The recommendation for augmentation in depressive patients is 2.5&nbsp;mg (or possibly 5&nbsp;mg) three times daily.
==See Also==


==References==
*[[Antiarrhythmic agents]]
*[[Beta blocker]]


{{Reflist|2}}
{{beta blockers}}


[[Category:Antiarrhythmic agents]]
[[Category:Beta blockers]]
[[Category:Cardiovascular Drugs]]
[[Category:Cardiovascular Drugs]]
[[Category:Beta blockers]]
[[Category:Drugs]]
[[Category:Drugs]]

Revision as of 19:44, 8 July 2014

Sotalol
BETAPACE® FDA Package Insert
Indications and Usage
Dosage and Administration
Contraindications
Warnings and Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Overdosage
Description
Clinical Pharmacology
Clinical Studies
How Supplied/Storage and Handling
Labels and Packages
SOTALOL HYDROCHLORIDE®
FDA Package Insert
Indications and Usage
Dosage and Administration
Dosage Forms and Strengths
Contraindications
Warnings and Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Overdosage
Description
Clinical Pharmacology
Nonclinical Toxicology
Clinical Studies
How Supplied/Storage and Handling
Patient Counseling Information
Labels and Packages
Clinical Trials on Sotalol
ClinicalTrials.gov
SandboxAlonso
Clinical data
Pregnancy
category
  • US: B (No risk in non-human studies)
Routes of
administration		oral
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability>95%
MetabolismNot metabolised
Elimination half-life12 hours
ExcretionRenal
Lactic (In lactating females)
Identifiers
CAS Number
PubChem CID
E number{{#property:P628}}
ECHA InfoCard{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
FormulaC12H20N2O3S
Molar mass272.3624 g/mol

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

For patient information about Sotalol, click here.

Synonyms / Brand Names: BETAPACE, SOTALOL HYDROCHLORIDE

Overview

Sotalol (trade names Betapace and Betapace AF, Berlex Laboratories) is a drug used in individuals with rhythm disturbances (cardiac arrhythmias) of the heart, and to treat hypertension in some individuals.

Category

Beta Blockers

FDA Package Insert

BETAPACE (sotalol hydrochloride) tablet

Indications and Usage | Dosage and Administration | Contraindications | Warnings and Precautions | Adverse Reactions | Drug Interactions | Use in Specific Populations | Overdosage | Description | Clinical Pharmacology | Clinical Studies | How Supplied/Storage and Handling | Labels and Packages

SOTALOL HYDROCHLORIDE injection

Indications and Usage | Dosage and Administration | Dosage Forms and Strengths | Contraindications | Warnings and Precautions | Adverse Reactions | Drug Interactions | Use in Specific Populations | Overdosage | Description | Clinical Pharmacology | Nonclinical Toxicology | Clinical Studies | How Supplied/Storage and Handling | Patient Counseling Information | Labels and Packages

Pharmacology

It falls into the class III antiarrhythmic agents because it inhibits the inward potassium ion channels in the heart. It is also a beta blocker because of its primary action on the β-adrenergic receptors in the heart.

By blocking the potassium channels, sotalol prolongs repolarization, therefore lengthening the QT interval and decreasing automaticity.

It also slows atrioventricular (AV) nodal conduction (beta-blocking effect).

Sotalol is a racemic mix of D and L enantiomers. The L-isomer is a beta blocker.

Sotalol is not selected for its beta-blocking ability, but rather for its Class III (potassium blocking) properties.

Indications

Sotalol is used to treat ventricular tachycardias as well as atrial fibrillation. Betapace AF is specifically labeled for atrial fibrillation.

Some evidence suggests that sotalol should be avoided in the setting of decreased ejection fraction due to heart attack.

References

See Also

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