DRUG PROFILE

Nifedipine [1]
Submitted to:
Dr.Imran Masood
(Assistant Professor IUB)
Group: 10
Roll No: 46, 47, 48, 49, 50, and 57
Brand Names:
Procardia, Procardia XL, Adalat CC, Nifedical
XL, Adalat, Afeditab CR, Nifediac CC
Pharmacological Class:
Calcium Channel Blockers, Dihydropyridine
STRUCTURE:

Dosage form and Strength:

Capsule:
10mg, 20mg
Tablet :( extended release)
30mg, 60mg
Routes of administration:
By mouth, topical
Administration:

Take on empty stomach

Mechanism of action:
Calcium-channel blocker; inhibits transmembrane
influx of extracellular calcium ions across myocardial and
vascular smooth muscle cell membranes without changing
serum calcium concentrations; this results in inhibition of
cardiac and vascular smooth muscle contraction, thereby
dilating main coronary and systemic arteries
Vasodilation with decreased peripheral resistance and
increased heart rate
PHARMACOKINETICS:
Absorption:
Bioavailability: Conventional, 40-77%; extended release,
65-89%
Onset: Conventional, 20 min; extended release, 30 min
Duration: Conventional, 8 hr; extended release, 24 hr
Peak plasma time: Conventional, 30-120 min; extended
release, 6 hr (Procardia XL) or 2.5-5 hr (Adalat CC)
Distribution:
Protein bound: 92-98, Vd: 1.42-2.2 L/kg
Metabolism:
Metabolized in liver by CYP3A4
Metabolites: Nitropyridine analogue (inactive)
Elimination:
Half-life: Conventional, 2-5 hr; 7 hr in cirrhosis
Dialyzable: No dose adjustments necessary in HD or PD
Excretion: Urine (60-80%), feces (20-40%)
Therapeutic uses
Angina:
10 mg (conventional) PO q8hr or 30-60 mg
(extended release) PO once daily initially; may be
increased every 7-14 days PRN
Maintenance: 10-20 mg (conventional) PO q8hr up to 20-
30 mg PO q6-8hr; not to exceed 180 mg/day
(conventional) or 120 mg/day (extended release)
Hypertension:
30-60 mg (extended release) PO once daily;
may be increased every 7-14 days PRN; not to exceed 90
mg/day (Adalat CC) or 120 mg/day (Procardia XL)
Pulmonary Hypertension:
30 mg (extended-release) PO q12hr; may be
increased to 120-240 mg/day (monitor)
Raynaud Phenomenon: (Off-label)
30-120 mg (extended release) PO once daily
Anal Fissures: (Off-label)
0.2% topical gel/ointment (extemporaneously
compounded) q12hr for 3-6 weeks 20 mg sublingual

Hypertension: (Off-label)
0.25-0.5 mg/kg/day (extended release) PO in 1 or 2 daily
doses initially; not to exceed 3 mg/kg/day (120 mg/day
For Children:
Not FDA approved for children
Potential toxic dose in children <6 years: 2 mg/kg
Dosing Modifications:
Peritoneal dialysis (PD):
Supplemental dose not necessary
Cirrhosis:
Consider dose adjustment
Adverse Effects:
Adverse effects differ between short-acting
(conventional) and extended-release formulations, with the
conventional preparations having more serious adverse
drug reactions in some cases
>10%
 Peripheral edema (10-30%)
 Dizziness (23-27%)
 Flushing (23-27%)
 Headache (10-23%)
 Heartburn (11%)
 Nausea (11%)
1-10%
 Muscle cramps (8%)
 Mood change (7%)
 Nervousness (7%)
 Cough (6%)
 Dyspnea (6%)
  Palpitations (6%)
 Wheezing (6%)
 Hypotension, transient (5%)
 Urticaria (2%)
 Pruritus (2%)
 Constipation (<2%)
 Chest pain (<2%)
Contraindications:
1. Hypersensitivity to nifedipine or other calcium-channel
blockers
2. Cardiogenic shock
3. Concomitant administration with strong CYP3A4
inducers (eg, rifampin, rifabutin, phenobarbital,
phenytoin, carbamazepine, St John's wort)
significantly reduces nifedipine efficacy
4. Immediate release preparation (sublingually or orally)
for urgent or emergent hypertension
Precautions:
1. Use with caution in (≤4 weeks) myocardial infarction
(MI), congestive heart failure (CHF), advanced aortic
stenosis, peripheral edema, symptomatic
hypotension, unstable angina, concurrent use of beta
blockers, hepatic or renal impairment, persistent
progressive dermatologic reactions, and exacerbation
of angina.
2. Short-acting nifedipine may be less safe than other
calcium-channel blockers in management of angina,
hypertension, or acute MI
 3. Use cautiously in combination with quinidine
4. Conventional (short-acting) form not indicated for
hypertension
5. Use extended-release form with caution in severe GI
stenosis; rare reports of GI obstructive symptoms in
patients with known strictures or without history of GI
obstruction in association with ingestion of long-acting
nifedipine;
6. Extended-release form contains lactose; thus,
patients with rare hereditary problems of galactose
intolerance, Lapp lactase deficiency, or glucose-
galactose malabsorption should not take this
medicine
7. Avoid use in heart failure due to lack of benefit, and/or
worse outcomes with calcium channel blockers in
general
8. Use with caution with hypertrophic in patients
cardiomyopathy and outflow tract obstruction;
reduction in afterload may worsen symptoms
associated with this condition
9. Avoid use of immediate release formulation in the
elderly; may cause hypotension and risk precipitating
myocardial ischemia

Pregnancy & Lactation

Pregnancy category: C
 Lactation: Drug is distributed into breast milk;
manufacturer suggests discontinuing drug or refraining
from nursing (however, American Academy of Pediatrics
states that drug is safe for nursing)
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant
women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk
but human studies not available or animal studies showed
minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal
studies show risk and human studies not available or
neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no
safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh
potential benefits. Safer alternatives exist.