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Nifedipine use, Side Effects, Mechanism of action, Dosage and Adverse effect

What is Nifedipine?

Nifedipine tablets belongs to the group of medicines called calcium channel blocking agents. IUPAC name of this drug is dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate. This drug is yellow in color and crystalline powder and insoluble in water.
Nifedipine tablets use for high blood pressure
Nifedipine tablets

Nifedipine tablets is a calcium channel blocker that blocks calcium to the muscles wall of the heart, allow the muscles to relax and widen to increase blood flow to the heart; making it easier for the heart to pump and function properly.
Nifedipine is widely used to treat
Hypertension
High blood pressure
Chronic stable angina
Ruptured aneurysm (a problem caused by a burst blood vessel around the brain)
Early labour for pregnant women
Raynaud’s phenomenon
Anal fissures
High altitude pulmonary edema
Spasms of esophagus due to cancer or tetanus
Pulmonary hypertension
This medicine is most frequently use for the treatment of high blood pressure or angina (chest pain).

Nifedipine Side Effects

Like other medicine nifedipine show some side effects, some side effects are more dangerous and some are very common. If you have facing any serious side effect immediately inform the doctor or pharmacist.
The common side effects are given bellow.
Bleeding, tender or swollen
Fast or irregular heartbeats
Feeling dizzy
Flushing
Headache
Hives
Itching
Loss of energy
Muscle pain
Nausea
Numbness in hand and feet
Rash
Swelling of the ankles or legs
Trembling
Visual disturbances
Nifedipine rapidly lower the blood pressure so patients are feels dizzy or faint after taking some dose and some time tachycardia may occurs.
Patient are not take this medicine along with grape fruits because it increase the bioavailability of nifedipine and also inhibit the cytochrome enzyme.
There are more comm0n side effects are palpitation, flushing, ankle edema, hypotension, headache, drowsiness and nausea.

Mechanism of action

Nifedipine  is calcium channel blockers (CCB)  and it belongs to group of dihydropyridine which is lipophilic drug. This drug is blocks L-type of voltage sensitive ca2+ channel. It like to bind with alpha subunit and helps to restrict all the calcium ions into vascular smooth muscle.
Nifedipine reduce the blood pressure by relaxing and expanding the blood vessel so blood flow is normal. This medicine is also good for angina which is helps for the relaxing or expanding the arteries so blood supply to heart is good.
Nifedipine structure
Nifedipine structure



How does Nifedipine work ?

Nifedipine blocks certain channels in blood vessels that cause relaxation of blood vessel . This results in a lowering of blood pressure and an increased blood flow to the heart, resulting in less chest pain.
Nifedipine help to inhibit calcium ion influx (slow-channel blocker or calcium ion antagonist)These drug has prominant smooth muscle relaxat action which is use for postpone the labour pain. Due to less concentration of calcium ion vasodilation occurs so arterial blood pressure gradually decrease. 
This medicine is helps to block influx of ca2+ so uterine contraction is properly functioning.

Pharmacokinetics of nifedipine

This medicine is well absorbed in gastrointestinal tract and it also show plasma level after given by sublingual, oral or rectal from. And its oral bioavailiability is about 56% to 77%. When patient take 10 mg of tablets plasma concentration of nifedipine is 111-210 mg/liter after 30-60 minutes. After 8 hour plasma concentration is drop down to 3.4 mg/liter.
This drug are eliminated from the body by hepatic metabolism and break down of two different chemical consttuents known as 1) 2,6-dimethyl-4-(2-nitrophenyl)-5-methoxycarbonyl-pyridine-3-carboxylic acid and 2) 2-hydroxymethyl-pyridinecarboxylic acid.

Adverse effects of Nifedipine

There are some medicine or drug which are reduce the effect of nifedipine like
Rifampicin (use for lepprosy)
Phenytoin (use for the epilepsy)
Carbamazepine
Phenobarbital
Some drug or medicine are increase the effect of nifedipine like
Macrolide antibiotics (erythromycin, clarithromycin, azithromycin are use for the infection)
Anti HIV Protease inhibitors (ritonavir, indinavir)
Azole antifungal (ketoconazole, itraconazole, fluconazole )
Fluoxetine and Nefazodone
Quinupristin and Dalfopristin
Cisapride
Valproic acid
Cimetidine
Betablocking medicine (propranolol or atenolol) are use for the treating heart attack or high blood pressure.
Don’t give the digoxin along with this medicine because the nifedipine reduce the clearance of the digoxin so over dose may happen.
Quinidine are use for the increase the heart beat, but this medicine are reduce the effect of quinidine so don’t take quinidine along with nifedipine.
At the time of organ transparent mostly doctor are prescribe tacrolimus to suppress immune system, but this medicine increase the effects of tacrolimus so reduce the dose of tacrolimus.

Pregnancy and breast-feeding

There are no major effects on the pregnant women but you contact your doctor at the time of take this drug if you are pregnant or breast feeding.
Nifedipine 10 mg tablets
Nifedipine 10 mg tablets

Dose of nifedipine

Always take this medicine according to doctor prescribe if doctor not advice the procedure or dose then ask for the properly. Take the tablets with glass of water.
Adult dose is starting form 30 mg tablets taken once in a day. Dose of the drug are increase upto 90 mg once in a day according to seriousness of disease. Take the dose in the morning time everyday.
Children below 18 year age group are not take this medicine because still date there are no information for the children dose.
Don’t take recovery dose if you forgot the dose previously.
Initial dose for the hypertension 30-60 mg tablet are taking once in a day. Maintenance dose is 30-90 mg orally once in day. Maximum dose up to 120 mg per day. Dose of nifedipine may increase gradually after taking the medicine 7 to 14 days.

What are the use of nifedipine cream?

Nifedipine cream or ointment are use for the treatment of anal fissures. This cream are helps to relax the smooth muscle around the anus and promotes the blood flow which is helps to heal fissure. This cream are helps to reduce anal canal pressure which leads to reduce the pain and spasm. In a day 3 time applied the cream for the treatment of fissures.

Reference: Pharmacokinetics and metabolism of nifedipine, Wikipedia.

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