Cilnidipine

Heart failure.

Patient with severe aortic stenosis, hypertrophic cardiomyopathy, outflow tract obstruction. Avoid abrupt withdrawal. Severe hepatic impairment. Elderly.

Significant: Angina, MI, reflex tachycardia; peripheral oedema (dose dependent). Rarely, symptomatic hypotension (with or without syncope).
Blood and lymphatic system disorders: Thrombocytopenia.
Cardiac disorders: AV block, extrasystoles.
Eye disorders: Dry eye syndrome, eye pain.
Gastrointestinal disorders: Gingival hyperplasia, nausea, vomiting, diarrhoea, heartburn, abdominal pain, abdominal distention, stomach discomfort, constipation, epigastric distress.
General disorders and administration site conditions: Lethargy, malaise, shivering.
Hepatobiliary disorders: Jaundice.
Investigations: Abnormal creatine kinase levels, ECG abnormality, abnormal LFTs.
Nervous system disorders: Headache, dizziness.
Psychiatric disorders: Insomnia, amnesia.
Renal and urinary disorders: Proteinuria, urinary frequency, urine sedimentation abnormality.
Skin and subcutaneous tissue disorders: Rash, pruritus, rubor, photosensitivity.
Vascular disorders: Hyperaemia, facial flushing.

This drug may cause dizziness and syncope, if affected, do not drive or operate machinery.

Monitor blood pressure and heart rate. Assess for signs of peripheral oedema.

Symptoms: Dizziness, nausea, slurred speech, confusion, irregular heartbeat, difficulty in breathing. Management: Symptomatic treatment.

Enhanced therapeutic effect with cimetidine and azole antifungal agents (e.g. miconazole, itraconazole).

Increased therapeutic effect with grapefruit juice.

May cause falsely elevated spectrophotometric values of urinary vanillylmandelic acid. May cause a false-negative aldosterone/renin ratio (ARR).

Description:
Mechanism of Action: Cilnidipine is a dihydropyridine Ca channel blocker. It inhibits Ca influx from L-type voltage-gated Ca channels in vascular smooth muscles thereby causing a decrease in peripheral vascular resistance and blood pressure. Additionally, it blocks the release of norepinephrine from sympathetic nerve endings through the inhibition of Ca influx from N-type voltage-gated Ca channels in sympathetic nerve endings, thus preventing the increase in heart rate during blood pressure-lowering events.
Pharmacokinetics:
Absorption: Absorbed from the small intestine. Time to peak plasma concentration: 1.8-2.2 hours.
Metabolism: Metabolised in the liver by the CYP3A4 and partially by the CYP2C19 isoenzymes.
Excretion: Via faeces (80%); urine (20%). Elimination half-life: 7.5 hours.

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5282138, Cilnidipine. https://pubchem.ncbi.nlm.nih.gov/compound/Cilnidipine. Accessed Oct. 24, 2023.

Store below 30°C.

Calcium Antagonists

C08CA14 - cilnidipine ; Belongs to the class of dihydropyridine derivative selective calcium-channel blockers with mainly vascular effects. Used in the treatment of cardiovascular diseases.

Anon. Cilnidipine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/07/2023.

Buckingham R (ed). Cilnidipine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/07/2023.

Cildine (Ajanta Pharma Phil). MIMS Philippines. http://www.mims.com/philippines. Accessed 04/07/2023.