ADALAT ® is a drug based on Nifedipine
THERAPEUTIC GROUP: Calcium antagonist - mainly vascular effect
Indications ADALAT ® Nifedipine
ADALAT ® is a drug indicated in the treatment of arterial hypertension and hypertensive crises, ischemic heart disease and angina pectoris.
Furthermore, ADALAT ® can also be used in vascular disorders such as those seen in Raynaud's syndrome.
Mechanism of action ADALAT ® Nifedipine
Nifedipine, the active ingredient of ADALAT ® taken orally, is absorbed very quickly and almost completely in the intestine, so as to guarantee a maximum plasma peak between 30 and 60 minutes. Although the absorption is very high, the bioavailability it is generally around 50%, given the first pass effect characterized by oxidation and the consequent inactivation of the active principle. The biologically active share acts on the surface of smooth muscle cells, inhibiting the activity of slow calcium channels. These channels are responsible for the massive entry of calcium into the intracellular environment, necessary to ensure all the series of events that underlie the contraction of these cells.
The "muscle relaxant" action is mainly carried out at the level of the muscle fiber cells of the coronary arteries and peripheral resistance vessels, while the heart muscle seems to be less affected and even less the skeletal muscle, which presents excitation-contraction mechanisms supported by calcium ions already present inside specific intracellular organelles. The biological action of nifedipine results in vasodilation and a decrease in peripheral resistance, with a consequent reduction in blood pressure, cardiac work and oxygen demand. All this justifies the therapeutic actions for which ADALAT is used.
Once its action ends after 2-3 hours, nifedipine is eliminated mainly by the kidney.
Studies carried out and clinical efficacy
1. OLMESARTAN MEDOXOMIL ON CARDIOVASCULAR HEALTH
1.NIFEDIPINE: VASCULAR ACTION
Hypertension. 2010 Aug; 56: 247-52. Epub 2010 Jun 7.
Nifedipine inhibits vascular smooth muscle cell dedifferentiation via downregulation of Akt signaling.
Kaimoto T, Yasuda O, Ohishi M, Mogi M, Takemura Y, Suhara T, Ogihara T, Fukuo K, Rakugi H.
The therapeutic efficacy of nifedipine is essentially due to the ability to block the calcium channels expressed on the surface of smooth muscle cells, preventing their contraction. However, recent molecular studies are further characterizing the biological action of this active ingredient, which seems to be able to inhibit the "expression of some factors necessary for the cellular differentiation of smooth muscle cells, thus preventing muscle thickening of the vessel.
2. EFFECTIVENESS AND SAFETY OF NIFEDIPINE
Rev Med Liege. 2005 Jan; 60: 61-3.
ACTION: The clinical study of the month
Piérard LA.
This study, conducted on more than 7500 patients, demonstrates how the administration of nifedipine even at doses of 60 mg / day can guarantee a reduction in cases of heart failure, up to 29%, and in the need for coronary angiography without the appearance of clinically relevant side effects.
3. NIFEDIPINA AND HYPERTENSIVE CRISIS
Cardiol Rev. 2010 Mar-Apr; 18: 102-7.
Hypertensive crisis.
Rodriguez MA, Kumar SK, De Caro M.
Hypertensive crisis is a very frequent and dangerous condition for the health of internal organs, characterized by systolic blood pressure values above 180mmHg or diastolic values above 120mmHg. Nifedipine, taken by sub-lingual administration, is one of the most used drugs in these cases, since it guarantees a good pressure return, with high efficacy. Despite the availability of several drugs on the market, scientists around the world still question the efficacy and safety of this clinical practice, which should only be used in case of real need, after considering the potential benefits and related costs.
Method of use and dosage
ADALAT ® nifedipine 10 mg capsules: for the treatment of arterial hypertension it is generally recommended to take 1 capsule 3 times a day.
The same basic dosages are maintained for the treatment of ischemic heart disease and Raynaud's syndrome, while in case of hypertensive crisis it may be necessary to take a chewed capsule before being swallowed, although this practice is still somewhat discussed for the possible side effects, even serious ones.
Although the aforementioned dosages are suggested, therapy with ADALAT ® is subject to significant variations in terms of useful and effective dose, which should be personalized by the doctor based on individual needs and the severity of the disease in progress.
Taking ADALAT ® should be preferred on an empty stomach, as pharmacokinetic studies have shown that food can increase the time it takes to reach the maximum plasma peak.
IN ANY CASE, BEFORE TAKING ADALAT ® Nifedipine - YOU MUST BE PRESCRIBED AND CHECKED BY YOUR DOCTOR.
ADALAT ® Nifedipine warnings
The administration of ADALAT ® should be carried out with particular care in case of concomitant administration of antihypertensive drugs or in case of patients with marked hypotension, as sudden and marked drops in blood pressure could compromise the patient's health.
Monitoring of blood glucose levels should be performed in the case of diabetic patients, and in the event of drug-induced hyperglycemia, therapy should be discontinued.
The dosage of ADALAT ® should be reviewed in case of hepatic insufficiency, given the first pass effect which halves the biologically effective dose, while the discontinuation of therapy should be done gradually in order to avoid rebound reactions.
Important drops in blood pressure, adaptation reactions to therapy in the initial phase, and the different individual susceptibility to nifedipine, could make the use of machinery and driving cars dangerous.
PREGNANCY AND BREASTFEEDING
The intake of ADALAT ® during pregnancy is strongly discouraged. This recommendation is based on several studies that show the series of teratogenic, mutagenic, fetotoxic and embryotoxic effects of nifedipine. The alteration of the normal embryonic and fetal development, as well as a "action" of the active ingredient, could also be determined by the impairment of normal uterine blood flow.
Nifedipine is secreted to a small extent also in breast milk, with effects on the newborn not yet characterized; therefore, it is advisable not to take the drug or to stop breastfeeding in case of real need.
Interactions
The simultaneous intake of other drugs could alter the normal pharmacokinetic and pharmacodynamic properties of ADALAT ®, resulting in a different biological efficacy.
More precisely, the interaction with:
- antihypertensive drugs of various kinds, could make the hypotensive effect more marked;
- Rifampicin, could accelerate the metabolism of nifedipine reducing its effectiveness;
- Grapefruit juice, with inhibition of hepatic enzymes responsible for the metabolism of nifedipine and consequent increase in its action;
- Digoxin, could cause a reduction in its clearance and an increase in plasma levels.
Even if not directly tested, it is possible that all other inhibitors and inducers of cytochromes, including alcohol, may alter the normal pharmacokinetic properties of nifedipine, compromising its efficacy and safety.
Contraindications ADALAT ® Nifedipine
ADALAT ® is contraindicated in case of hypersensitivity to one of its components, in case of cardiovascular shock and marked aortic stenosis. The immediate release formula is also contraindicated in case of angina or recent myocardial infarction.
Undesirable Effects - Side Effects
The various clinical trials show a good tolerability of the drug, with clinically insignificant and transient adverse reactions. Among the most complained symptoms it is possible to find dizziness, muscle cramps, myalgia, cough and gastro-enteric symptoms.
However, it should be remembered that, although very rare, some adverse reactions - clinically more important - can occur in particular categories of patients at risk, or in the case of drug interactions, and cause hyperkalimia, renal insufficiency, impaired liver function and thrombocytopenia.
The drug appears to be well tolerated and cases of hypersensitivity are rare, mainly manifesting themselves with gastrointestinal and cutaneous symptoms.
Note
ADALAT ® can only be sold under medical prescription.
The information on ADALAT ® Nifedipine published on this page may be out of date or incomplete. For a correct use of this information, see the Disclaimer and useful information page.
