NEET MDS Lessons
Pharmacology
Calcium Channel Blocking Agents
• Act on contractile and conductive tissues of the heart and on vascular smooth muscles
• Prevent movement of extracellular calcium into the cell
– Coronary and peripheral arteries dilate
– Myocardial contractility decreases
– Depress conduction system
Therapeutic Actions
• Inhibit movement of calcium ions across the membranes of myocardial and arterial muscle cells. Altering the action potential and blocking muscle cell contraction
• Depress myocardial contractility
• Slow cardiac impulse formation in the conductive tissues
• Cause a fall in BP
Angiotensin
It is generated in the plasma from a precursor plasma globulin. It is involved in the electrolyte balance, plasma
volume and B.P
Angiotensin I:
Renin is an enzyme produced by the kidney in response to a number of factors including adrenergic activity (β1-
receptor) and sodium depletion. Renin converts a circulating glycoprotein (angiotensinogen) into an inactive material angiotensin-I. It gets activation during passage through pulmonary circulation to angiotensin II by (ACE). ACE is located on the luminal surface of capillary endothelial cells, particularly in the lungs & also present in many organ (e.g brain).
Angiotensin II:
Is an active agent, has a vasoconstrictor action on blood vessels & sodium and water retention
Phenobarbital (Luminal): for generalized tonic-clonic and partial seizures (not used for absence seizures)
Mechanism: enhances GABA inhibition (↑ open time of Cl channels in presence of GABA)
Side effects: sedation, ataxia, cognitive impairment, induction of hepatic microsomal enzymes
On the basis of Receptors, drugs can be divided into four groups,
a. agonists
b. antagonists
c. agonist-antagonists
d. partial agonists
a. Agonist
morphine fentanyl pethidine
Action : activation of all receptor subclasses, though, with different affinities
b. Antagonist
Naloxone , Naltrexone
Action : Devoid of activity at all receptor classes
c. Partial Agonist: (Mixed Narcotic Agonists/Antagonists)
Pentazocine, Nalbuphine, Butorphanol , Buprenorphine
Action: activity at one or more, but not all receptor types
With regard to partial agonists, receptor theory states that drugs have two independent properties at receptor sites,
a. affinity
The ability, or avidity to bind to the receptor
Proportional to the association rate constant, Ka
b. efficacy
or, intrinsic activity, and is the ability of the D-R complex to initiate a pharmacological effect
Drugs that produce a less than maximal response and, therefore, have a low intrinsic activity are called partial agonists.
These drugs display certain pharmacological features,
a. the slope of the dose-response curve is less than that of a full agonist
b. the dose response curve exhibits a ceiling with the maximal response below that obtainable by a full agonist
c. partial agonists are able to antagonise the effects of large doses of full agonists
Ketoprofen
It acts by inhibiting the body's production of prostaglandin.
Fifth Generation:
These are extended spectrum antibiotics.
Ceftaroline, Ceftobiprole
Levofloxacin
Levofloxacin is effective against a number of gram-positive and gram-negative bacteria. Because of its broad spectrum of action, levofloxacin is frequently prescribed in hospitals for pulmonary infections