Cilnipine
Cilnipine Uses, Dosage, Side Effects, Food Interaction and all others data.
Cilnipine acts on the L-type calcium channels of blood vessels by blocking the incoming calcium and suppressing the contraction of blood vessels, thereby reducing blood pressure. Cilnipine also works on the N-type calcium channel located at the end of the sympathetic nerve, inhibiting the emission of norepinephrine and suppressing the increase in stress blood pressure.
Administration of cilnidipine has been shown to present an antisympathetic profile in vitro and in vivo. It decreases blood pressure safely and effectively without excessive blood pressure reduction or tachycardia.
| Trade Name | Cilnipine |
| Generic | Cilnidipine |
| Cilnidipine Other Names | Cilnidipine |
| Type | Tablet |
| Formula | C27H28N2O7 |
| Weight | Average: 492.528 Monoisotopic: 492.18965125 |
| Protein binding | Cilnidipine presents a very high protein binding that represents to even 98% of the administered dose. |
| Groups | Investigational |
| Therapeutic Class | Calcium-channel blockers |
| Manufacturer | Jubilant Life Sciences |
| Available Country | India |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Cilnipine is used for the management of hypertension for end-organ protection. It is reported to be useful in elderly patients and in those with diabetes and albuminuria. Cilnipine has been increasingly used in patients with chronic kidney disease.
Hypertension is the term used to describe the presence of high blood pressure. The blood pressure is generated by the force of the blood pumped from the heart against the blood vessels. Thus hypertension is caused when there is too much pressure on the blood vessels and this effect can damage the blood vessel
Cilnipine is also used to associated treatment for these conditions: High Blood Pressure (Hypertension)
How Cilnipine works
Cilnipine acts on the L-type calcium channels of blood vessels by blocking the incoming calcium and suppressing the contraction of blood vessels, thereby reducing blood pressure. Cilnipine also works on the N-type calcium channel located at the end of the sympathetic nerve, inhibiting the emission of norepinephrine and suppressing the increase in stress blood pressure.
Dosage
Cilnipine dosage
5-10 mg once daily, increase to 20 mg once daily if necessary.
Side Effects
Dizziness; flushing; headache; hypotension; peripheral oedema; tachycardia; palpitations; GI disturbances; increased micturition frequency; lethargy; eye pain; depression; ischaemic chest pain; cerebral or myocardial ischaemia; transient blindness; rashes; fever; abnormal liver function; gingival hyperplasia; myalgia; tremor; impotence.
Toxicity
The percentage of reports of cilnidipine that express drug toxicity reported as side effects are 5.26%.
Precaution
Hypotension, poor cardiac reserve, heart failure. Sudden withdrawal may exacerbate angina. Discontinue in patients who experience ischemic pain following administration. Pregnancy, lactation.
Interaction
Other antihypertensives; aldesleukin; antipsychotics that cause hypotension; may modify insulin and glucose responses; quinidine; carbamazepine; phenytoin; rifampicin; cimetidine; erythromycin.
Volume of Distribution
Drugs on the group of dihydropyridines such as cilnidipine tend to have a large volume of distribution.
Elimination Route
Cilnipine presents a very rapid absorption with a maximum peaked concentration after 2 hours. Its distribution tends to be higher in the liver as well as in kidneys, plasma and other tissues. Cilnipine does not present a high accumulation in the tissue after repeated oral administration.
Cilnipine is reported to present very low bioavailability determined to be approximately 13%. This low bioavailability is suggested to be due to its low aqueous solubility and high permeability. Hence, efforts have been made in order to find an innovative formulation that can significantly improve the bioavailability of this drug. One of these formulations corresponds to the generation of polymeric nanoparticles which enhance the bioavailability by 2.5-3-fold.
Half Life
The half-life of the hypotensive effect for cilnidipine is of about 20.4 min.
Elimination Route
Cilnipine gets eliminated through the urine in a proportion of 20% of the administered dose and 80% is eliminated by the feces.
Pregnancy & Breastfeeding use
No specific information about USFDA pregnancy category. Caution should be exercised during Cilnipine use in pregnancy. Nursing mothers should consult a physician before taking Cilnipine.
Contraindication
Cardiogenic shock; recent MI or acute unstable angina; severe aortic stenosis.
Innovators Monograph
You find simplified version here Cilnipine
Cilnipine contains Cilnidipine see full prescribing information from innovator Cilnipine Monograph, Cilnipine MSDS, Cilnipine FDA label
FAQ
What is the use of Cilnipine?
Cilnipine used to treat high blood pressure (hypertension). It belongs to a class of medicines known as a calcium channel blocker which helps to lower blood pressure. This helps prevent heart attacks and strokes. It may also be prescribed to prevent angina (heart-related chest pain). Cilnipine is approved for use in Japan, China, India, Nepal, Korea, and some European countries to treat hypertension.
Is Cilnipine safe?
It has been reported that once-daily administration of cilnidipine resulted in a safe and more effective BP decrease in essential hypertension without excessive BP reduction or reflex tachycardia than similar administration than once-daily administration of nifedipine (14) or nisoldipine (15).
How does Cilnipine work?
Cilnipine work by decreases blood pressure. Due to its blocking action at the N-type and L-type calcium channel, cilnidipine dilates both arterioles and venules, reducing the pressure in the capillary bed.
What are the common side effects of Cilnipine?
The side effects could be severe dizziness, fast heartbeat, and swelling of face, lips, tongue, eyelids, hands and feet.
Is Cilnipine safe during pregnancy?
Cilnipine is not rendered 'safe' for use during pregnancy. Hence, it should not usually be used during pregnancy because other relatively safer alternatives to control blood pressure are available.
Is Cilnipine safe during breastfeeding?
Cilnipine passes into breast milk in amounts that are probably too small to be harmful to a nursing infant. It's generally considered safe to breastfeed while taking Cilnipine. No adverse effects have been reported in breastfed babies.
Can I drink alcohol with Cilnipine ?
Cilnipine may cause a decrease in blood pressure so avoid alcohol while using this medicine.
Can I drive after taking Cilnipine?
Consumption of Cilnipine may cause dizziness. Avoid activities like driving while on this medication.
When should be taken of Cilnipine?
Cilnipine Tablet can be taken anytime of the day. Usually, it is advised to be taken in the morning, but your doctor may advise to take it in the evening as well. You should take it at the same time each day so that you remember to take it and consistent levels of medicine are maintained in the body.
How Cilnipine should be taken?
Cilnipine comes in the form of a tablet and to be taken orally either once daily or as directed by the physician.
Can I take Cilnipine on an empty stomach?
This Cilnipine can be taken either before or after meals.
How long does Cilnipine take to work?
Cilnipine starts to work on the day you start taking it, but it may take a couple of weeks fully take effect. If you're taking nifedipine for high blood pressure, you may not have any symptoms. In this case, you may not feel any different when you take it.
How long does Cilnipine stay in my system?
The elimination half-life of Cilnipine is approximately two hours.
Can I take Cilnipine for a long time?
Usually, treatment with Cilnipine is long term, even for the rest of your life.
Who should not take Cilnipine?
You should not use Cilnipine if you have severe coronary artery disease, or if you have had a heart attack within the past 2 weeks.
What happen If I stop taking Cilnipine?
Talk to your doctor if you want to stop taking Cilnipine. Stopping Cilnipine may cause your blood pressure to rise – and this may increase your risk of heart attack and stroke. If you're bothered by side effects, your doctor may be able to prescribe you a different medicine.
What happen If I overdose on Cilnipine?
Taking too much of this drug may cause severe side effects such as very low blood pressure (hypotension), a dangerously slow heart rate (bradycardia), heart failure, trouble breathing, extreme tiredness, dizziness, or very low blood sugar that could even lead to a coma. If you take too much nebivolol, call your doctor or go to the nearest hospital emergency department right away.
What happen If I missed Cilnipine?
If you forget to take your dose, take it as soon as you remember, unless you remember just a few hours before the time for your next dose. Then only take one dose. Never try to catch up by taking two doses at once. This could result in dangerous side effects.
Can Cilnipine affects my heart ?
Cilnipine may inhibit increases in heart rate and QT interval. Cilnipine may have beneficial effects in reducing cardiovascular events, resulting from increased sympathetic nerve activity and lethal arrhythmias in hemodialysis patients.
Can Cilnipine affect my kidneys?
Cilnipine effectively reduces the low- grade albuminuria in hypertensive CKD patient but main adverse effect of this drug induces the ankle edema, pedal edema, and peripheral edema.
