NAME:SAMRA SHOUKAT

MSC(PREVIOUS)
SEAT NO:P19241023
 Calcium is essential for muscle contraction.
Due to the movement of calcium from
extracellular to intracellular muscles get
contract specially smooth muscles or
arterioles. Due to this contraction movement
of blood toward the heart tissue are slow
which oxygen supply is low which is the
main reason of angina. The calcium channel
blocker protect the tissue by inhibiting the
entrance of calcium into cardiac and smooth
muscles of the coronary and systemic
arterial bed.
 They are classified into two classes.
 1) Dihydropyridine.
 2)Non- Dihydropyridine.
 DYHYDROPYRIDINE:
 Dihydropyridine ca+2 channel blocker are
derived from the molecule dihydropyridine.
 They are mostly used to reduced systemic
vascular resistance and arterial pressure.
 Sometimes they are used to treat angina.
  Examples of dihydropyridine are :
 Amlodipine(Norvasc)
 Aranidipine(Sapresta)
 Lacidipine(MOTENS,Lacipil)Lercanidipine(Zani
dip)
 Manidipine(Calslot,cardenSR)
 Nicardipine(Cardene,carden)
 Nifidipine(procardia,Adalat)
 Nimodipine(Nimotop)
  NON
– DIHYROPYRIDINE:
 PHENYLALKYLAMINE:

The Phenylalkylamine class of ca+2 calcium

blocker mainly affects the cell of the heart.
 They have negative choronotropic effects.
 They have minimal vasodialatory effects
compared with dihydropyridine.
 Example are: Verapamill etc.
  BENZOTHIAZEPINE :
 It belongs to the molecule Benzothiazepine.
 These drugs are intermediate class between
dihydropyridine and phenylalkylamine.
 They have both cardiac depressor and
vasodialatorn action.
 Calcium Channel:
 Voltage Sensitive Channel: Activate when
potential drop to -40mv
 Receptor Operated: Activated by –Androgen
and other agonist
 Independent of membrane depolarization
 Leak channel:
 Leak Channel: small amount of Ca+2 leak
into resting cell and pump out by Ca+2
ATPase Mechanical strecth allow it.
 MECHANISM OF ACTION:
 Calcium voltage channels are of 3 sub types.
 L-Type
 T-Type
 N-Type
 L-Type in cardiac and smooth muscle type
  Ca+2 channel Blocker

Bind L-Type Ca+2 Channel

Prevent entry of Ca+2 into cell

1)Artereolar Dialation
 2)Myocardial conc HR
 FOC

 Result Myocardial workload

  SIDE EFFECTS:
 Dizziness, headache
 Fluid build up
 Facial redness
 Constipation
 Altered heart rate
 Hypertension
 EFFECTS:
 They are effective in
treating hypertension in
patients with angina or
diabetes

 High dosage of short

acting calcium channel
blockers should be avoided
because of increased risk
of myocardial infarction
due to excessive
vasodialation.
 Trade Name: Norvasc
 It is a medication used for the treatment of
hypertension and coronary artery disease.
 It is also used in stable angina.
 MECHANISM OF ACTION:
 It produces coronary vasodialation by
inhibiting the entry of calcium ions into the
voltage gated channel the vascular smooth
muscles and myocardium during
depolarization.
 It decreases cardiac work, decrease cardiac
oxygen consumption.
 INDICATIONS:
 Hypertensions, Stable angina.
 AVAILABILITY; It ia available in tablets 2.5,5
or 10mg
 SIDE EFFECTS:
 Dizziness, light -headednedss
 ,headache, asthenia,fatigueand abdominal
pain
 Nitrates are medication used for treating or
preventing heart pain (angina, chest pain)
caused by heart disease, usually of the arteries
in the heart.
 treat by decreased workload of the heart
by causing vasodialation.
 MECHANISM OF ACTION:
 Nitroglycerine or other nitrate drug release
nitrate ions these ions are converted to nitric
oxide by enzymes in the blood (is a
hydrophobic gas) that in diffuses in the blood
into the inside neighboring smooth muscle cell.
 Inside the smooth muscle cell nitric oxide activate the
enzyme Guanylyl cylase. Which then convert GTP in the
cyclic GMP.
 Cyclic GMP then activates cGMP dependent protein
kinase which phosphorylase myosin light chain
kinase(MLCK) and also phosphorylase the SERCA pump
 Phosphorylation inhibits (MLCK)s so phosphorylase lies
the mysosin chain less phosphorylation of (MLCK) does
not happen then less myosin /interaction therefore
smooth muscle relaxation .
 The serca pump is activated by cyclic AMP dependent
protein kinase this act to decrease calcium in the
cytosol also leading to relaxation
  EFFECTS:
 Relaxes blood vessel walls
 Dialates coronary arteries.
 Reduced workload to heart.

 USES:
 Inthe management of angina
pectoris.
 Heart failure
:
 Examples;
 EXAMPLES OF
NITRATES ARE
 sublinIsosorbide
dinitrate(solids)
 Isosorbide
mononitrate(solids)
 Nitroglycerine
(moderatly Volactile)
 Amyl nitrite(volatile)
 Nitroglycerine sublingual tablet is a prescriiption
drug available at the name nitrostat.
 Nitoglycerine also cames as a spray solution
 Niroglycerine is used to treat angina(Chest
pain)Angina is a pain or discomfort that happens
when part of your heart does not get enough
blood. It can happen in your chest ,neck ,arm and
lower jaw.
 Nitroglycerine belongs to a class of drugs called
vasodialators. A class of drugs is a group of
medication that work in a similar way. These
drugs are often used to treat similar conditions
 Nitroglycerine works by relaxing the smooth
muscle and blood vessels in your blood
  SIDE EFFECTS::
 Headache
 Dizziness
 Weakness
 Fast heart rate
 Nausea
 Vomiting
 Rash