Metoprolol (Tartrate)
Metoprolol (Tartrate) is a cardioselective ß-blocking agent with intrinsic sympathomimetic activity. Metoprolol (Tartrate) is approximately equipotent to propranolol in inhibiting ß1 receptors such as those in heart but 50 to 100 fold less potent than propranolol in blocking ß2 receptors. Drugs that blocks the ß1 receptor have been developed to eliminate the unwanted bronchoconstrictor effects (ß2) of propranolol seen among the asthmatic patients. Metoprolol antagonizes ß1 receptors at doses 50 to 100 times less than those required to block ß2 receptors. This cardioselectivty is more pronounced at low doses and is lost at high doses. It lowers the blood pressure in hypertension. It slows the heart rate. Metoprolol (Tartrate) is prepared by chemical synthesis and the racemate is used clinically. Metoprolol (Tartrate) is adminsitered orally and intravenously.
Primary Characteristics
It is of Synthetic origin and belongs to Amino propanolol.
It belongs to Beta-1 adrenergic antagonist pharmacological group on the basis of mechanism of action and also classified in Beta Blocker, Beta1 Selective pharmacological group.
Molecular Weight: 684.8 · pKa: 9.5 · Solubility in Water: very high · Solubility in Alcohol: soluble · Non-proprietary name: Metoprolol (Tartrate).
Pharmacokinetics
Absorption: Metoprolol (Tartrate) has an oral bioavailability is 25% (±25%), pre-systemic (first-pass) metabolism accounts for 50% (±10%).
Distribution: Metoprolol (Tartrate) has a volume of distribution is 3-6 l/kg. plasma protein binding is 12%.
Elimination: it is metabolised via extensive by Liver, plasma half-life is 3-7 hr, renal excretion is >95%.
Advertisement
Indications
Metoprolol (Tartrate) is primarily indicated in conditions like Angina, Cardiac arrhythmia, Hypertension, Hyperthyroidism (adjunct), Maintenance of recurrent duodenal ulcers, Migraine prophylaxis, Myocardial infarction, Prevention of relapse in duodenal ulcer, Severe or recurrent duodenal and gastric ulcertion, Surgery, To prevent recurrence of neural tube defect.
Metoprolol (Tartrate) is also indicated for secondary conditions like Thyrotoxicosis.
Contraindications
Metoprolol (Tartrate) is contraindicated in conditions like Cardiogenic shock, Bradycardia, Atrioventricular block, Refractory heart failure.
Dosage
Metoprolol (Tartrate)'s dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 5 mg | 5 mg | — | IV | For Cardiac Arrythmia rate is 2mg/min may be repeated at intervals of 5 min to a total dose of 10-15 mg .Maintainence therapy dose should not exceed than 50 mg (PO) given 3 times a day ,4 to 6 hrz after IV therapy |
| 18.75 mg | 18.75 mg | — | PO | In management of symptomatic heart failure. |
| 75 mg | 75 mg | Every 12h | PO | For Angina Pectoris For emergency treatment. |
| 150 mg | 150 mg | — | PO | Migtaine prephylaxi''s |
| 150 mg | 150 mg | Every 24h | PO | For Hypertension Initially given 100 mg.Maintainance dose is 200 mg Can be increased up to 400 mg |
| 175 mg | 175 mg | Every 8h | PO | For Cardiac Arrythmia |
| Paediatric Dosage (20kg) | ||||
| 3.25 mg/kg | 3.25 mg/kg | Every 12h | Oral | - |
| Neonatal Dosage (3kg) | ||||
| No data. | ||||
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
Metoprolol (Tartrate) in overdosage may give rise to further complications which include Hyperglycemia , Agranulocytosis , Severe bradycardia .
Metoprolol (Tartrate) produces potentially life-threatening effects which include Myocardial depression. Careful monitoring is needed with proper medical management.
The signs and symptoms that are produced after acute overdosage of Metoprolol (Tartrate) are Bradycardia, Hypotension.
Metoprolol (Tartrate) is known to cause more or less tolerable side effects which are usually transient. These include Alopecia, Diarrhea, Dizziness, Dyspnea, Elevation of liver enzymes, Extremities coolness, Fatigue, GI upset, Hyperpigmentation , Lassitude , Musculoskeletal pain , Nausea, Pruritus , Sleep pattern disturbances, Vomiting , Xerosis.
Warnings / Precautions
Available Brands
Storage Conditions
Drug Classification
- 1.12.3.1 — Beta blocking agents