Nifedipine

Registered South African indications:

• Hypertension
• Angina pectoris

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Breastfeeding (XL tab, SR tab, SR cap)
• Hepatic impairment (XL tab, SR tab, SR cap)
• Clinically significant aortic stenosis
• Cardiogenic shock
• Unstable angina
• Inflammatory bowel disease (XL tab)
• Crohn's disease (XL tab)
• History of gastrointestinal obstruction (XL tab)
• Oesophageal obstruction (XL tab)
• Decreased diameter of gastrointestinal lumen (XL tab)
• Secondary prevention of myocardial infarction
• Myocardial infarction <1 month
• Kock pouch (XL tab, SR cap)
• Malignant hypertension
• Coadministration with rifampicin
• Acute porphyria (Certain slow-/controlled-/sustained-release products: check individual package insert)

Cautions

• Pregnancy
• Breastfeeding (cap)
• Moderate to severe hepatic impairment (cap) 
• Elderly (cap)
• Hypotension
• Poor cardiac reserve
• Impaired left ventricular function
• Diabetes mellitus
• Hypovolaemia
• Dialysis
• Galactosaemia (XL tab, SR tab, SR cap)
• Lapp lactase deficiency (XL tab, SR tab, SR cap)
• Glucose-galactose malabsorption (XL tab, SR tab, SR cap)

Forms avail. in SA and covered in this monograph: sustained release tab (SR tab), cap, controlled release tab (XL tab), sustained release cap (SR cap), retard tab (Ret tab)

Hypertension - mild to moderate

• Oral (SR cap): 10-40mg, 12hrly
• Oral (XL tab, SR tab): 30-90mg, dly; Max: 120mg/24hrs
• Oral (Ret tab): 20-40mg, 12hrly; Max 80mg/24hrs

Chronic stable angina pectoris

• Oral (cap): 5-20mg, 8hrly; Max: 60mg/24hrs
• Oral (SR cap): 10-40mg, 12hrly
• Oral (XL tab, SR tab): 30-90mg, dly; Max: 120mg/24hrs
• Oral (Ret tab): 20-40mg, 12hrly; Max 80mg/24hrs

Hypertensive emergency in pregnancy (BP >160/110)

• Oral (cap): 10mg, immediately; Repeat after 30min if systolic BP >160 or diastolic BP >110

Preterm labour - gestation <34 weeks

• Oral (cap): 20mg, immediately; If contractions persist, give 10mg after 30min; Thereafter: 10mg, 4hrly for up to 24hrs

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SR cap, Ret tab, tab: Gradual discontinuation recommended especially at higher doses

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Ret tab, XL tab: Do not cut/crush/chew/dissolve

Not established for use in children below 18 years

Pregnancy

• Caution
• Nifedipine should not be used during pregnancy unless the clinical conditions of the woman require treatment with nifedipine. Safe use of nifedipine during human pregnancy has not been established. Animal studies have shown reproductive toxicity (embryotoxic, foetotoxic and teratogenic effects) at maternally toxic doses
• From the clinical evidence available a specific prenatal risk has not been identified, although an increase in perinatal asphyxia, caesarean delivery, prematurity and intrauterine growth retardation have been reported. It is unclear whether these reports are due to underlying hypertension, its treatment or to a specific drug effect
• Acute pulmonary oedema has been observed when calcium channel blockers, among others nifedipine, have been used as a tocolytic agent during pregnancy, especially in cases of multiple pregnancies (twins or more), with the intravenous route and/or concomitant use of beta-2-agonists
• Available information is inadequate to rule out adverse drug effects on the unborn and newborn child. Any use in pregnancy requires very careful risk-benefit assessment and should only be considered if all other treatment options are not indicated or have failed to be efficacious

Breastfeeding

• Oral (cap): Caution; not recommended
• Oral (XL tab, SR tab, SR cap): Contraindicated
• Nifedipine passes into breast milk and nifedipine controlled release formulations are contraindicated for use in breastfeeding mothers as there is no experience of possible effects on infants
• The nifedipine concentration in the milk is almost comparable with mother serum concentration. For immediate release formulations, it is proposed to delay breastfeeding or milk expression for 3-4 hours after drug administration to decrease the nifedipine exposure to the infant

Fertility

• In single cases of in vitro fertilisation, calcium antagonists like nifedipine have been associated with reversible biochemical changes in the spermatozoa's head section that may result in impaired sperm function
• In those men who are repeatedly unsuccessful in fathering a child by in vitro fertilisation, and where no other explanation can be found, calcium antagonists like nifedipine should be considered as a possible cause

Renal Impairment

• No dose adjustment recommended

Hepatic Impairment

• Oral (cap): Mild (Child-Pugh class A): No dose adjustment recommended
• Oral (cap): Moderate to severe (Child-Pugh class B and C): Caution; dose adjustment recommended
  Initial: 10mg, 8hrly; Up-titrate gradually over 7-14 days; Maintenance: 30-90mg/day in 3 divided doses; Max: 90mg/24hrs 
• Oral (XL tab, SR tab, SR cap): Contraindicated

Elderly

• Oral (cap): Caution; dose adjustment recommended
  Elderly population tend to experience a greater hypotensive response or constipation
  Initial: 5-10mg, 12hrly; Up-titrate to 30-60mg/day in 2 divided doses over 2-4 weeks; Max (for chronic use): 120mg/24hrs  
• Oral (XL tab, SR tab, SR cap): No dose adjustment recommended

Porphyria Information

• Probably not porphyrinogenic (PNP)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Anxiety reactions
• Sleep disorders
• Mood changes
• Headache
• Vertigo
• Nervousness
• Migraine
• Tremor
• Dysaesthesia
• Somnolence

Cardiovascular Disorders

• Tachycardia
• Palpitations
• Cardiovascular disease
• Angina pectoris
• Oedema
• Hypotension
• Posternal Hypotension
• Syncope

Respiratory Disorders

• Nose bleed
• Nasal congestion
• Dyspnoea
• Pulmonary oedema

Gastrointestinal Disorders

• Oesophagitis
• Constipation
• Nausea and vomiting
• Dyspepsia
• Flatulence
• Diarrhoea
• Dry mouth
• Gingival hyperplasia
• Gingivitis
• Bezoar
• Dysphagia
• Intestinal obstruction
• Intestinal ulcer
• Gastroesophageal sphincter insufficiency

Hepatobiliary Disorders

• Transient increase in liver enzymes
• Jaundice
• Hypersensitivity type jaundice

Genitourinary Disorders

• Eruction
• Polyuria
• Nocturia
• Dysuria
• Erectile dysfunction

Endocrine and Metabolic Disorders

• Anorexia
• Hyperglycaemia

Musculoskeletal Disorders

• Muscle cramps
• Joint swelling
• Arthralgia
• Myalgia
• Unspecified pain

Skin and Subcutaneous Tissue Disorders

• Erythema
• Pruritus
• Sweating
• Toxic epidermal necrolysis
• Photosensitivity allergic reaction
• Exfoliative dermatitis
• Palpable purpura

Immune, Blood and Lymphatic System Disorders

• Agranulocytosis
• Leucopenia
• Angioedema
• Pruritus
• Urticaria
• Rash
• Anaphylactic reactions
• Fever

Sensory Disorders

• Visual disturbances
• Eye pain

Others

• Weight loss

• Rifampicin
• Antihypertensives
• Beta blockers
• Magnesium sulphate
• CYP3A4 inhibitors
• CYP3A4 inducers
• Barium contrast
• Grapefruit juice
• Cimetidine
• Quinidine
• Digoxin
• Diltiazem
• Non-polarising muscle relaxants
• Cisapride
• Quinupristin

None routine

Capsule 5mg - EML (Hospital)

Tablet 10mg, 30mg, XL 30mg, XR 60mg, XL 60mg - EML (Primary)

Drug-Laboratory Interactions

• A false-positive effect may be experienced when performing a barium contrast x-ray

Nifedipine is a potent calcium antagonist of the 1,4-dihydropyridine type. It inhibits calcium influx through the cell membrane of cardiac and smooth muscle cells in the coronary and peripheral circulation. This results in peripheral vasodilation and thus a reduction in peripheral resistance and increased myocardial oxygen delivery.

Capsule 5mg

• Bio-Nifedipine (Biotech Laboratories)
• Cardifen (Litha)

Capsule 10mg

• Bio-Nifedipine 10 (Biotech Laboratories)
• Cardifen (Pharmacare) Discontinued: 01/04/2018
• Rolab-Nifedipine (Sandoz)

Capsule sr 20mg

• Adco-Vascard 20 SR (Adcock)

Capsule sr 30mg 

• Adco-Vascard 30 SR (Adcock) originator

Capsule 60mg 

• Adco-Vascard 60 (Adcock)

Tablet retard 10mg

• Adalat Retard (Bayer) originator

Tablet retard 20mg

• Adalat Retard (Bayer) originator
• Cipalat Retard (Cipla)

Tablet cr 30mg

• Gitsalat (Bayer) originator

Tablet cr 60mg 

• Gitsalat (Bayer) originator

Tablet sr 30mg

• Fedaloc 30 SR (Pharma Dynamics)
• Macorel 30 SR (Specpharm)
• Spec Nifedipine 30 SR (Specpharm)

Tablet sr 60mg

• Fedaloc 60 SR (Pharma Dynamics)
• Macorel 60 SR (Specpharm)
• Spec Nifedipine 60 SR (Specpharm)

Tablet xl 30mg

• Adalat XL (Bayer) originator
• Bio Nifedipine XL (Biotech Laboratories)
• Cipalat XR (Cipla)
• Fidocare 30 XL (Biotech Laboratories)

Tablet xl 60mg

• Adalat XL (Bayer) originator
• Bio Nifedipine XL (Biotech Laboratories)
• Cipalat XR (Cipla)
• Fidocare 60 XL (Biotech Laboratories)