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HTN Case No.6 Amlodipine and Cilnidipine

Amlodipine_লেগ_ইডিমা_হয়, Cilnidipine_এ_কেন_হয়না?

এইটা বুঝতে হলে দুইটার মেকানিজম অফ একশন বুঝতে হবে- দুইটা যদিও ক্যালসিয়াম চ্যানেল ব্লকার, তবে কিছুটা প্রার্থক্য আছে–

Amlodipine হচ্ছে L-type CCB

Cilnidipine হচ্ছে L and N type CCB.

L -type calcium চ্যানেল থাকে ব্লাড ভেসেল + হার্টে–

L-type Calcium channel Active থাকলে blood vessel constriction এর মাধ্যমে বিপি বেড়ে যায়-

তাই Amlodipine দিয়ে L-Type calcium channel block হলে Blood vessel dilate হয়, ব্লাড ভেসেল ডায়ালেটের মাধ্যমে প্রেশার কমে-

Blood vessel dilate হয়ে প্রেশার নরমালের চেয়েও কমে যায়, তখন হোমিওস্ট্যাসিস মেইনটেইন করার জন্য Heart rate বেড়ে যায়, পেশেন্ট এর ট্যাকিকার্ডিয়া হয়, ব্লাড প্রেশার কমে যাওয়ার ফলে প্রেশার বাড়ানোর জন্য হার্ট রেট বেড়ে যাওয়ার প্রক্রিয়াকে Reflex tachycardia বলে-

আবার Amlodipine Arterial dialation এর পরে এখানে ফ্লুইডের পরিমান বেড়ে যায়, কিছু ফ্লুইড তখন ভেসেল থেকে লিক হয়ে টিস্যুতে চলে আসে, কারণ amlodipine Arteriole ডাইলেট করলেও venules dilate করেনা, তাই capillary hydrostatic pressure বেড়ে ফ্লুইড ভেসেল থেকে বেরিয়ে চলে আসে–

পায়ে ফ্লুইড জমে কেনো?

leg এ ফ্লুইড জমার কারণ হচ্ছে gravitional force..

তাহলে Cilnidipine ও switch করে কি লাভ—-

হ্যাঁ, কিছুটা লাভ আছে,

Cilnidipine হচ্ছে Both L type and N type calcium channel blocker.

N-type calcium channel থাকে নিউরোনের মধ্যে– cilnidipine শুধু কেবল ব্লাড ভেসেল + হার্টেই কাজ করেনা, এসবের সাথে সাথে এইটা নার্ভাস সিস্টেমেও কাজ করে-

N-Type channel block করার মাধ্যমে cilnidipine Sympathetic activity কমায়, তাই ক্যালসিয়াম চ্যানেল ব্লকার রিফ্লেক্স ট্যাকিকার্ডিয়া করলেও cilnidipine এ Reflex tachycardia হয়না—

আবার Cilnidipine যেমন ভাবে artery dilate করে, একইভাবে venous dilation করে, তাই এখানে সেই পরিমান ফ্লুইড লিকেজ হয়না, যে পরিমান ফ্লুইড লিকেজ amlodipine এ হয়ে থাকে—-

সেইজন্য amlodipine এ যেমন Reflex tachycardia +leg oedema হয়, Cilnidipine এ তা হয়না-

সিনারিও-

রেহানা ৬০ বছর বয়স, HTN diagnosis হয়েছে ৩ মাস আগে, ডাক্তার ওনাকে amlodipine 5 mg. দিয়েছেন, এতে করে ওনার প্রেশার কন্ট্রোলে আছে, তবে ওনার leg Oedema হচ্ছে, যাতে ওনার অসুবিধা হচ্ছে, করনীয় কি?

উত্তর- Amlodipine এ সাধারণত leg oedema হয়, এতে পেশেন্ট এর লাইফ স্টাইলে কোনো সমস্যা না হলে এইটাই চলবে, আর life style এ সমস্যা হলে পেশেন্ট কে cilnidipine এ switch করে দিবেন-

Amlodipine 5 mg এর Equivalent হচ্ছে cilnidipine 10 mg…

Amlodipine:-

Tablet 1:-

Amdocal 10mg (AS A Amlodipine Besilate AS A Calcium-channel blockers).

Indications of Amdocal 10mg (AS A Amlodipine Besilate AS A Calcium-channel blockers).

 

Essential hypertension: Amdocal is efficacious as monotherapy in the treatment of hypertension. It may be used in combination with other antihypertensive agents.

Angina pectoris: Amdocal is indicated for the treatment of chronic stable angina pectoris and is efficacious as monotherapy. It may be used in combination with other antianginal agents.

Vasospastic angina: Amdocal is indicated for the treatment of confirmed or suspected vasospastic angina. It may be used as monotherapy or in combination with other antianginal drugs.

Pharmacology Amdocal 10mg (AS A Amlodipine Besilate AS A Calcium-channel blockers).

Amlodipine is a dihydropyridine calcium-channel blocker, with a long duration of action, used for the treatment of hypertension and angina pectoris. Amlodipine influences the myocardial cells, the cells within the specialized conducting system of the heart, and the cells of vascular smooth muscle. Administration of Amlodipine results primarily in vasodilation, with reduced peripheral resistance, blood pressure and afterload, increased coronary blood flow and a reflex increase in coronary heart rate. This in turn results in an increase in myocardial oxygen supply and cardiac output.

Dosage & Administration Amdocal 10mg (AS A Amlodipine Besilate AS A Calcium-channel blockers).

Hypertension: Usual dose is 5 mg once daily. The maximum dose is 10 mg once daily. Elderly patients with hepatic insufficiency may be started on 2.5 mg once daily; this dose may also be used when adding Amlodipine to other antihypertensive therapy.

Angina (Chronic stable or Vasospastic): 5 to 10 mg, using the lower dose for elderly and in patients with hepatic insufficiency. Most patients require 10 mg.

Administrations: May be taken without regard to meals.

Interaction Amdocal 10mg (AS A Amlodipine Besilate AS A Calcium-channel blockers).

Drug Interactions-

  • Potentially hazardous interactions: Little or no data are available in patients with markedly impaired cardiac left ventricular function; however, as with other calcium antagonist drugs, the combination of Amdocal and p-blockers should be avoided in such patients.

Other Significant Interactions-

  • Digoxin: Absence of any interaction between Amdocal and Digoxin in healthy volunteers has been documented in a controlled clinical study.
  • Cimetidine: An unpublished clinical study indicated no interaction between, Amdocal and Cimetidine in healthy volunteers.
  • Warfarin: An unpublished clinical study in healthy volunteers indicates that Amdocal did not significantly alter the effect of Warfarin on prothrombin time.
  • Food: Food does not alter the rate or extent of absorption of Amdocal.

Contraindications

Hypersensitivity to dihydropyridine derivatives. Pregnant woman.

Side Effects Amdocal 10mg (AS A Amlodipine Besilate AS A Calcium-channel blockers).

The most common adverse effects of amlodipine are associated with vasodilatory action, such as dizziness, flushing, headache, hypotension and peripheral edema. Gastrointestinal disturbances, increased micturition frequency, lethargy, eye pain and mental depression may also occur. A paradoxical increase in ischaemic chest pain may occur at the start of the treatment and in a few patients excessive fall in blood pressure has led to cerebral or myocardial ischaemia or transient blindness. Rashes, fever and abnormalities in liver function due to hypersensitivity reaction of Amdocal may occur.

Pregnancy & Lactation Amdocal 10mg (AS A Amlodipine Besilate AS A Calcium-channel blockers).

Pregnancy Category C. There are no adequate and well-controlled studies of Amlodipine in pregnant women. Amlodipine should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. It is not known whether Amlodipine is excreted in human milk. In the absence of this information, it is recommended that nursing be discontinued while Amlodipine is administered.

Precautions & Warnings

Precaution should be taken in patients with hepatic impairment and during pregnancy and breast feeding.

Use in Special Populations Amdocal 10mg (AS A Amlodipine Besilate AS A Calcium-channel blockers).

Children with hypertension from 6 years to 17 years of age: 2.5 mg once daily as a starting dose, up-titrated to 5 mg once daily if blood pressure goal is not achieved after 4 weeks. Doses in excess of 5 mg daily have not been studied in pediatric patients.

Children under 6 years old:  The effect of amlodipine on blood pressure in patients less than 6 years of age is not known.

Elderly: Amdocal used at similar doses in elderly or younger patients is equally well tolerated. Normal dosage regimens are recommended in the elderly, but increase of the dosage should take place with care.

Renal impairment: Changes in amlodipine plasma concentrations are not correlated with degree of renal impairment, therefore the normal dosage is recommended. Amdocal is not dialysable.

Hepatic impairment: Dosage recommendations have not been established in patients with mild to moderate hepatic impairment; therefore dose selection should be cautions and should start at the lower end of the dosing range. The pharmacokinetics of Amdocal have not been studied in severe hepatic impairment. Amdocal should be initiated at the lowest dose (2.5 mg once daily) and titrated slowly in patients with severe hepatic impairment.

Overdose Effects Amdocal 10mg (AS A Amlodipine Besilate AS A Calcium-channel blockers).

Symptoms: Available data suggest that large overdosage could result in excessive peripheral vasodilatation and possibly reflex tachycardia. Marked and probably prolonged systemic hypotension up to and including shock with fatal outcome have been reported.

Management: Clinically significant hypotension due to amlodipine overdosage calls for active cardiovascular support including frequent monitoring of cardiac and respiratory function, elevation of extremities, and attention to circulating fluid volume and urine output. 

A vasoconstrictor may be helpful in restoring vascular tone and blood pressure, provided that there is no contraindication to its use. Intravenous calcium gluconate may be beneficial in reversing the effects of calcium channel blockade. Gastric lavage may be worthwhile in some cases. In healthy volunteers the use of charcoal up to 2 hours after administration of amlodipine 10 mg has been shown to reduce the absorption rate of amlodipine. Since amlodipine is highly protein-bound, dialysis is not likely to be of benefit.

Therapeutic Class Amdocal 10mg (AS A Amlodipine Besilate AS A Calcium-channel blockers).

Calcium-channel blockers

Cilnidipine:-

Tablet 2.Duocard 10 mg (AS A Cilnidipine AS A Calcium-channel blockers).

Indications of Tablet:-Duocard 10 mg (AS A Cilnidipine AS A Calcium-channel blockers).

 

Duocard is indicated 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. Duocard 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.

Pharmacology of Tablet:-Duocard 10 mg (AS A Cilnidipine AS A Calcium-channel blockers).

 

Cilnidipine is a dihydropyridine calcium-channel blocker. Cilnidipine binds to the dihydropy-ridine binding sites of the L-type voltage dependent calcium channel and inhibits Ca2+ influx across the cell membranes of vascular smooth muscle cells via this channel, consequently vascular smooth muscle is relaxed, causing vasodilation. Cilnidipine inhibits Ca2+ influx via N-type voltage dependent calcium channels in the sympathetic nerve cell membrane. The inhibition of Ca2+ influx via N-type voltage dependent calcium channel was observed over a similar range of drug concentrations to those inhibiting L-type voltage dependent Ca2+ channels. Consequently, release of norepinephrine from sympathetic nerve terminals would be inhibited. Cilnidipine is considered to suppress the reflex increase in heart rate after blood pressure reduction.

Dosage & Administration of Tablet:-Duocard 10 mg (AS A Cilnidipine AS A Calcium-channel blockers).

 

Adults: 5-10 mg once daily after breakfast. Maximum dose: 20 mg once daily.

Pediatric use: The safety of Cilnidipine in pediatric patients has not been established.

Elderly use: Since the elderly may be more susceptible to hypotension, therapy should be initiated with the lowest possible dose (5 mg).

Interaction of Tablet:-Duocard 10 mg (AS A Cilnidipine AS A Calcium-channel blockers).

 

Other anti-hypertensive, antipsychotics that cause hypotension, quinidine, carbamazepine, phenytoin, rifampicin, cimetidine, erythromycin.

Contraindications of Tablet:-Duocard 10 mg (AS A Cilnidipine AS A Calcium-channel blockers).

 

Cilnidipine is contraindicated in patients with known sensitivity to Cilnidipine or any of the excipients or patients having cardiogenic shock, recent MI or acute unstable angina and severe aortic stenosis.

Side Effects of Tablet:-Duocard 10 mg (AS A Cilnidipine AS A Calcium-channel blockers).

 

The most common side effects of Duocard are: Dizziness; flushing; headache; hypotension; peripheral oedema; palpitations; GI disturbances; increased micturition frequency; lethargy; eye pain; depression.

Pregnancy & Lactation of Tablet:-Duocard 10 mg (AS A Cilnidipine AS A Calcium-channel blockers).

 

Cilnidipine should not be administered in pregnant woman or woman having possibilities of being pregnant. It is also advisable to avoid the administration of Cilnidipine to nursing mothers. However, if the administration is indispensable, the patient should be instructed to discontinue lactation.

Precautions & Warnings of Tablet:-Duocard 10 mg (AS A Cilnidipine AS A Calcium-channel blockers).

 

Duocard should be administered with care in the following patients: patients with serious hepatic dysfunction, patients with a history of serious adverse reactions to calcium antagonists. During the discontinuation, the dosage should be gradually decreased under close observation.

Therapeutic Class of Tablet:-Duocard 10 mg (AS A Cilnidipine AS A Calcium-channel blockers).

 

Calcium-channel blockers

Raiyyan Tahsan Date:27-01-2025 Monday Time:6-02-2025

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