NORVASC
a. General description of the drug
Norvasc is a calcium channel blocker with a long duration of action that reduces
the transmembrane influx of calcium ions into vascular smooth muscle and cardiac
muscle. By blocking calcium ion flux, it dilates vascular smooth muscle directly.
b. Mechanism of Action
Norvasc is a dihydropyridine calcium antagonist that decreases the
transmembrane influx of calcium ions into vascular smooth muscle and cardiac
muscle. Amlodipine binds to both dihydropyridine and non-dihydropyridine binding
sites, according to experimental evidence. The contractile activities of cardiac
muscle and vascular smooth muscle are dependent on the entry of extracellular
calcium ions through particular ion channels. Amlodipine selectively inhibits calcium
ion influx across cell membranes, with a larger impact on vascular smooth muscle
cells than cardiac muscle cells. Negative inotropic effects are detectable in vitro but
have not been shown at therapeutic levels in intact animals. Amlodipine does not
influence serum calcium concentration. Within the physiological pH range,
amlodipine is an ionized molecule (pKa = 8.6), and its kinetic interaction with the
calcium channel receptor is characterized by a gradual association and dissociation
rate with the receptor binding site, resulting in a gradual beginning of effect.
c. Example of the drug (generic name)
Amlodipine besilate
d. Usage and usual dose
Hypertension: The majority of people can take amlodipine besylate as the only
medication to control their blood pressure. It is suggested for the first-line treatment of
hypertension. Amlodipine is given once daily in dosages ranging from 2.5 to 10 mg,
depending on the patient's blood pressure level.
Coronary Artery Disease: In individuals with coronary artery disease, amlodipine
besylate is recommended to lower the risk of coronary revascularization and the
requirement for hospitalization due to angina (CAD). 5 to 10 mg administered once daily
is the suggested dosage range. The majority of individuals in clinical investigations
needed 10 mg.
Chronic Stable Angina: For the first-line treatment of myocardial ischemia,
amlodipine besylate is recommended, regardless of whether the cause is a fixed
blockage (stable angina) or a vasospasm/vasoconstriction (Prinzmetal's or a variant
angina). Amlodipine is typically started at a dose of 5 mg once day, and depending on
how each patient responds, the amount may be increased to a maximum of 10 mg.
Use in Children: Pediatric patients aged 6 to 17 years should take 2.5 mg to 5 mg of an oral
antihypertensive once day. Pediatric patients have not been studied with doses greater than 5
mg per day.
e. Availability in the Philippines
Amlodipine besilate (Norvasc) is available with 5mg and 10mg each tablet which also comes
in brand-name versions called Katerzia. This drug costs at around Php. 25-35 depending on the
dosage and brand. However, a doctor's prescription is required to purchase this product.
References:
Norvasc Dosage & Drug Information | MIMS Philippines. (2022). Retrieved 24
November 2022, from [Link]
CARDIZEM
a. General description of the drug
Cardizem is an antihypertensive benzothiazepine derivative having vasodilator
characteristics. It functions by reducing the calcium influx into cardiac and vascular smooth
muscle during depolarization, among other modes of action.
b. Mechanism of Action
Excitation of cardiac muscle utilizes L-type slow calcium channels, which have a high
activation threshold and slow inactivation profile. Late phase pacemaker potential is driven by
L-type calcium channels. Activating L-type calcium channels permits calcium ions to enter
smooth and cardiac muscle during depolarization and excitement. This cation influx may also
stimulate intracellular calcium ion release. Diltiazem is a slow calcium channel blocker that
binds to the alpha-1C subunit's extracellular location, which is the S5-6 linker region of domain
IV and/or S6 segment of domain III. Diltiazem can access this binding site intracellularly or
extracellularly, although it requires voltage-induced membrane conformational changes.
Diltiazem prevents calcium from entering cardiac and vascular smooth muscle cells. In isolated
human atrial and ventricular myocardium, diltiazem decreased tension at calcium channel-
associated membrane potentials but had no effect at higher positive potentials. This impact
may be achieved by voltage-dependent obstruction of L-type calcium channels and suppression
of calcium ion release from ER stores, without affecting sodium-calcium coupled transport or
calcium sensitivity of myofilaments. Diltiazem has an ionotropic, energy-saving impact on the
myocardium by inhibiting inward calcium influx. Diltiazem inhibits slow channel activity, slowing
atrioventricular nodal conduction.
c. Example of the drug (generic name)
Diltiazem
d. Usage and usual dose
Ischemic Heart Disease
Adult: The first dose is 120 mg/day delivered preferably before meals and at bedtime;
the dosage should be increased gradually in equally divided doses (two to four times daily) at 1-
to 2-day intervals until the optimal response is achieved. The optimal dosage appears to be
between 180 mg and 360 mg per day. In some instances, up to 480 mg/day may be provided.
Hypertension
Adult: Doses must be individualized. Initial dose is 120 to 240 mg/day in divided doses
between meals and bedtime. Maximum antihypertensive effect is usually shown after 14 days
of chronic medication; modify dosage accordingly. 240 to 360 mg/day is typical.
Elderly: Initial dosing for modified-release capsules is 60 mg bid, with a gradual increase
to 240 mg once daily.
Use in Children: Safety and efficacy in pediatric patients have not been established.
f. Availability in the Philippines
Available doses are 30 milligrams (mg), 60 mg, 90 mg, or 180 mg table. Drug Price Reference
Index is Php.12.00. A doctor’s prescription is required to purchase this product.
