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Amlodipine (Norvasc)

Drugs & Medication

Amlodipine (Norvasc)

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Amlodipine chemical structure
Amlodipine
Systematic (IUPAC) name
3-ethyl-5-methyl-2-(2-aminoethoxymethyl)-4-(2-
chlorophenyl)-1,4-dihydro-6-methyl-3,5- pyridinedicarboxylate benzenesulfonate
Identifiers
CAS number 88150-42-9
ATC code C08CA01
PubChem 2162
DrugBank APRD00520
Chemical data
Formula C20H25ClN2O5.C6H6O3S
Mol. weight 408.879 g/mol
Pharmacokinetic data
Bioavailability 64 to 90%
Metabolism Hepatic
Half life 30 to 50 hours
Excretion Renal
Therapeutic considerations
Pregnancy cat. C(AU) C(US)
Legal status POM(UK) -only(US)
Routes Oral (tablets)

Amlodipine (as besylate, mesylate or maleate) is a long-acting calcium channel blocker used as an anti-hypertensive and in the treatment of angina. Amlodipine is marketed as Norvasc in North America and as Istin in the United Kingdom as well as under various other names. As other calcium channel blockers, amlodipine acts by relaxing the smooth muscle in the arterial wall, decreasing peripheral resistance and hence improving blood pressure; in angina it improves blood flow to the myocardium. It was developed under the direction of Dr. Simon Campbell.

Contents

Indications

  • hypertension
    prophylaxis of angina

Cautions

  • hepatic impairment
    pregnancy

Contra-indications

  • cardiogenic shock
    unstable angina
    significant aortic stenosis
    breast feeding

Side effects

Some side effects of the use of amlodipine may be:

  • Very often: peripheral edema (feet and ankles) - in 1 of 10 users
    Often: dizziness, palpitations, muscle, stomach or headache, dyspepsia, nausea - in 1 in 100 users
    Sometimes: blood disorders, development of breasts in men (gynecomastia), impotence, depression, insomnia, tachycardia - in 1 in 1,000 users
    Rarely: erratic behavior, hepatitis, jaundice - in 1 in 10,000 users
    Very rarely: hyperglycemia, tremor, Stevens-Johnson syndrome - in 1 in 100,000 users

Source: Sandoz product information sheet

Dose

  • Hypertension or angina: 5 or 10 mg once daily.

Salts

In the United Kingdom tablets of amlodipine from different suppliers may contain different salts. The strength of the tablets is expressed in terms of amlodipine base. i.e. without the salt. Tablets containing different salts are therefore considered interchangeable.

Patent Loss

Pfizer patent protection on Norvasc until 2007. [1]

External links


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