Calcium Channel Blockers Flashcards
How do calcium channel blockers work?
- have different affinities for different sites, hence different therapeutic effects
- interfere with inward displacement of calcium ions through slow channels of active cell membranes
Three different classes
1) Dihydropyridines
2) Phenylaklyamines
3) Benzothiazepines
Dihydropyridines CCB
EXAMPLES - Amlodpines, nifedipine (maintain same brand for MR), Lercanidipine, lacidipine and felodipine
- Relax vascular smooth muscle (predominantly vasodilators effects)
- Have no anti - arrhythmic activity
Phenylalkylamines eg. Verapamil (avoid in heart failure)
Verapamil:
- used to treat hypertension, angina,arrhythmias
- highly negatively inotrpic CCB so slow heart rate
- minimal vasodilators effects in comparison to Dihydropyridines
- causes constipation
- has profound cardiac depressant effects and may precipitate heart failure
- do not use with BB, causes bradycardia,hypotension - especially IV verapamil
Benzothiazepines - eg. Diltiazem (avoid in heart failure)
- have both cardiac depressant and vasodilatory effects
- intermediate between phenylalkylamines and Dihydropyridines
- effective in most forms of angina
- longer acting formulations used for hypertension
- may be used for patients where BB are contraindicated or ineffective
- less negative inotropic effect than verapamil
- use with caution with BB (because of risk of bradycardia)
Unstable Angina
CCB do not reduce the risk of myocardial infarction in unstable angina
- verapamil and diltiazem should be reserved for patients resistant to treatment with BB
- Sudden withdrawal of CCB may exacerbate angina
Prescribing and dispensing diltiazem
Different versions of MR preps containing more than 60mg may not have the same clinical effects
- prescribers need to prescribe as brand
Other anti-angina drugs - Nicorandil
Licensed for long term treatment of angina
Has both arterial and venous vasodilatory effects
Potassium channel activators with nitrate component
Other drugs - ivabadrine and ranolazine
Side effects of CCB
Vasodilatory effects
- dizziness
- flushing
-headaches
-postural hypotension
- GI disturbances
- Ankle swelling
- Skin reactions
!!!!!! Sudden withdrawal may exacerbate myocardial ischaemia!!!