Carvedilol
Carvedilol is a non-selective ß adrenoceptor blocking agent. Carvedilol is given as a racemic mixture. The S(-) isomer is a nonselective adrenoceptor blocking agent, but both S(-) and R(+) isomers have approximately equal a blocking potency. Carvedilol is used as a prophylaxis of stable angina and in the treatment of hypertension
Primary Characteristics
It is of Synthetic origin and belongs to Aminopropanol.
It is classified in Alpha-Beta Blocker pharmacological group.
Molecular Weight: 406.5 · pKa: 7.9 · Solubility in Water: insoluble · Solubility in Alcohol: sparingly · Non-proprietary name: Carvedilol.
Pharmacokinetics
Absorption: Carvedilol has an oral bioavailability is 40% (±40%), pre-systemic (first-pass) metabolism accounts for 70% (±10%).
Distribution: Carvedilol has a volume of distribution is 1.5-2 l/kg. plasma protein binding is > 95%.
Elimination: it is metabolised via extensively by Liver, plasma half-life is 4-8 hr, renal excretion is < 2% (unchanged).
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Indications
Carvedilol is primarily indicated in conditions like Adjunct in heart failure, Angina, Angina pectoris, Cardiac arrhythmia, Cardiomyopathy, Congestive heart failure, Essential hypertension, Hypertension, Sedation for surgical and diagnostic proceduers, Sedation in intensive care.
Carvedilol is also indicated for secondary conditions like Maintenance of anaesthesia, Myocardial infarction.
Contraindications
Carvedilol is contraindicated in conditions like Asthma, Cardiogenic shock, Hepatic dysfunction, Hypersensitivity.
Dosage
Carvedilol's dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 12.5 mg | 12.5 mg | Every 24h | PO | Initiallly. |
| 25 mg | 25 mg | Every 24h | PO | After 2-3 days. |
| Paediatric Dosage (20kg) | ||||
| 0 – 0 | — | — | — | Not Recommended in this Age Group |
| Neonatal Dosage (3kg) | ||||
| 0 – 0 | — | — | — | Not Recommended in this Age Group |
Drug Interactions
Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Side Effects
Carvedilol in overdosage may give rise to further complications which include Bradycardia , Postural hypotension , Bronchospasm .
Carvedilol produces potentially life-threatening effects which include AV block. Careful monitoring is needed with proper medical management.
The signs and symptoms that are produced after acute overdosage of Carvedilol are Severe bradycardia, Severe hypotension.
Carvedilol is known to cause more or less tolerable side effects which are usually transient. These include Dizziness, Syncope .
Warnings / Precautions
Available Brands
Storage Conditions
Drug Classification
- 1.12.3.1 — Beta blocking agents