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Calcium channel blockers or calcium channel antagonists or calcium antagonists are several medications that disrupt the movement of calcium (Ca 2+ ) through calcium channels. It is prescription medications that relax blood vessels and increase the supply of blood and oxygen to the heart while also reducing the heart’s workload. Calcium-channel blockers bind to L-type calcium channels located on the vascular smooth muscle, cardiac myocytes, and cardiac nodal tissue (sinoatrial and atrioventricular nodes). These channels are responsible for regulating the influx of calcium into muscle cells.
N-type, L-type, and T-type voltage-dependent calcium channels are present in the zona glomerulosa of the human adrenal, and CCBs can directly influence the biosynthesis of aldosterone in adrenocortical cells, with consequent impact on the clinical treatment of hypertension with these agents.CCBs have been shown to be slightly more effective than beta blockers at lowering cardiovascular mortality, but they are associated with more side effects. Potential major risks, however, were mainly found to be associated with short-acting CCBs.
Types of Calcium Channel Blockers
Dihydropyridine
Dihydropyridine (DHP) calcium channel blockers are derived from the molecule dihydropyridine and often used to reduce systemic vascular resistance and arterial pressure. This CCB class is easily identified by the suffix “-dipine”.
- Amlodipine
- Aranidipine
- Azelnidipine
- Barnidipine
- Benidipine
- Cilnidipine
- Clevidipine
- Efonidipine
- Felodipine
- Isradipine
- Lacidipine
- Lercanidipine
- Manidipine
- Nicardipine
- Nifedipine
- Nilvadipine
- Nimodipine This substance can pass the blood-brain barrier and is used to prevent cerebral vasospasm.
- Nisoldipine
- Nitrendipine
- Pranidipine
Non-dihydropyridine
- Fendiline
- Gallopamil
- Verapamil
Benzothiazepine
- Diltiazem (also used experimentally to prevent a pain, nausea, or light sensitivity. সহজ বাংলা: বারবার হওয়া বিশেষ ধরনের মাথাব্যথা।" data-rx-term="migraine" data-rx-definition="Migraine is a recurring headache disorder often with throbbing pain, nausea, or light sensitivity. সহজ বাংলা: বারবার হওয়া বিশেষ ধরনের মাথাব্যথা।">migraine)
Nonselective
While most of the agents listed above are relatively selective, there are additional agents that are considered nonselective. These include mibefradil, bepridil, flunarizine, fluspirilene, and fendiline.
Mechanism of Action of Calcium Channel Blockers
In the body’s tissues, the concentration of calcium ions (Ca2+) outside of cells is normally about 10000-fold higher than the concentration inside of cells. Embedded in the membrane of some cells are calcium channels. When these cells receive a certain signal, the channels open, letting calcium rush into the cell. The resulting increase in intracellular calcium has different effects in different types of cells. Calcium channel blockers prevent or reduce the opening of these channels and thereby reduce these effects. Several types of calcium channels occur, with a number of classes of blockers, but almost all of them preferentially or exclusively block the L-type voltage-gated calcium channel. Voltage-dependent calcium channels are responsible for excitation-contraction coupling of skeletal, smooth, and cardiac muscle and for regulating aldosterone and cortisol secretion in endocrine cells of the adrenal cortex. In the heart, they are also involved in the conduction of the pacemaker signals. CCBs used as medications primarily have four effects:
- By acting on vascular smooth muscle, they reduce contraction of the arteries and cause an increase in arterial diameter, a phenomenon called vasodilation(CCBs do not work on venous smooth muscle).
- By acting on cardiac muscles (myocardium), they reduce the force of contraction of the heart.
- By slowing down the conduction of electrical activity within the heart, they slow down the heart beat.
- By blocking the calcium signal on adrenal cortex cells, they directly reduce aldosterone production, which correlates to lower blood pressure.
Since blood pressure is in intimate feedback with cardiac output and peripheral resistance, with relatively low blood pressure, the afterload on the heart decreases; this decreases how hard the heart must work to eject blood into the aorta, so the amount of oxygen required by the heart decreases accordingly. This can help ameliorate symptoms of ischaemic heart disease such as angina pectoris.
Indications of Calcium Channel Blockers
- Chronic stable angina pectoris
- High blood pressure (hypertension)
- Raynaud’s syndrome
- Heart failure
- Angina pectoris prophylaxis
- Hypertensive emergency
- Hypertrophic cardiomyopathy
- Migraine prevention
- Premature labour
- Pulmonary edemas
- Pulmonary hypertension
- Ureteral ualculus
- Vasospastic angina
Contra Indications
- Porphyria
- The acute syndrome of the heart
- Severe narrowing of the aortic heart valve
- Severe heart failure
- Abnormally low blood pressure
- Kidney disease with a reduction in kidney function
- Fluid Retention in the Legs, arms or hands
- Blood circulation failure due to the serious heart condition
- Chronic idiopathic constipation
- Stomach or intestine blockage
- Narrowing of the intestines
- Decreased motility function of stomach or itestines
- Heart attack
- Allergies to calcium channel blockers
- Calcium channel blocking agents-dihydropyridines
Side Effects of Calcium Channel Blockers
The most common
- a severe headache, rapid heartbeat, stiffness in your neck,
- chest pain, fast or slow heart rate;
- swelling, rapid weight gain;
- Xerostomia (dry mouth)
- A headache
- Fatigue
- Skin reactions
- Hypotension
- Anxiety
- Constipation
- Nausea/vomiting
- Weight gain/loss
- Erectile dysfunction
More common
- Abdominal or stomach pain, discomfort, or pain when an area is touched or pressed. সহজ বাংলা: চাপ দিলে ব্যথা।" data-rx-term="tenderness" data-rx-definition="Tenderness means pain when an area is touched or pressed. সহজ বাংলা: চাপ দিলে ব্যথা।">tenderness
- chills or fever
- difficulty with moving
- headache, severe and throbbing
- joint or back pain
- muscle aching or cramping
- muscle pains or stiffness
- chest pressure or squeezing pain in chest
- discomfort in arms, shoulders, neck or upper back
- excessive sweating
- feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
- sudden tingling or coldness in an arm or leg
- sudden slow or difficult speech
- sudden drowsiness or need to sleep
- fast breathing
- sharp pain when taking a deep breath
- fast or slow heartbeat
- coughing up blood
- rust colored urine
- decreased amount of urine
Rare
- Anxiety
- change in vision
- chest pain or tightness
- confusion
- a cough
- Agitation
- arm, back, or jaw pain
- blurred vision
- chest pain or discomfort
- convulsions
- extra heartbeats
- fainting
- hallucinations
- a headache
- irritability
- lightheadedness
- mood or mental changes
- muscle pain or cramps
- muscle spasm or jerking of all extremities
- nervousness
Drug Interactions
Calcium-channel blockers may interact with the following drug, suppliments, & may change the efficacy of the drug
- allopurinol
- alpha blockers (e.g., alfuzosin, doxazosin, tamsulosin)
- alpha agonists (e.g., clonidine, methyldopa)
- angiotensin II receptor blockers (ARBs; e.g., candesartan, losartan)
- antidiabetes medications (e.g., insulin, metformin, glyburide)
- atypical anti-psychotics (e.g., clozapine, olanzapine, quetiapine, risperidone)
- azathioprine
- barbiturates (e.g., butalbital, pentobarbital phenobarbital)
- beta-adrenergic blockers (e.g., atenolol, propranolol, sotalol)
- “azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
- calcium channel blockers (e.g., amlodipine, diltiazem, nifedipine, verapamil)
- canagliflozin
- ciprofloxacin
- calcium supplements (e.g., calcium carbonate, calcium citrate)
- carbamazepine
- clopidogrel
- cyclosporine
- diuretics (water pills; e.g., furosemide, hydrochlorothiazide, triamterene)
- duloxetine
- “gliptin” insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।" data-rx-term="diabetes" data-rx-definition="Diabetes is a condition where blood sugar stays too high because insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।">diabetes medications (e.g., linagliptin, saxagliptin, sitagliptin)
- guanfacine
- heparin
- levodopa
- medications that increase potassium levels (e.g., potassium supplements, spironolactone, amiloride, and salt substitutes containing potassium)
- metformin
- nonsteroidal anti-inflammatory drugs (NSAIDs; e.g., ibuprofen, indomethacin, naproxen)
- other angiotensin-converting-enzyme inhibitors (ACEIs; e.g., captopril, ramipril)
- pentoxifylline
- macrolide antibiotics (e.g., clarithromycin, erythromycin)
- methylphenidate
- monoamine oxidase inhibitors (MAOIs; e.g., moclobemide, phenelzine, rasagiline,selegiline, tranylcypromine)
- phosphodiesterase-5 inhibitors (e.g., sildenafil, tadalafil, vardenafil)
- pregabalin
- sodium phosphates
- tizanidine
- trimethoprim
- valproic acid
- warfarin
References
