NEET MDS Lessons
Pharmacology
PSEUDOEPHEDRINE
Pseudoephedrine appears to have less pressor activity and weaker central nervous system effects than ephedrine. It has agonist activity at both β1 and β2 adrenoceptors, leading to increased cardiac output and relaxation of bronchial smooth muscle.
Pseudoephedrine is rapidly absorbed throughout the body. It is eliminated largely unchanged in urine by N-demethylation.
It is indicated in symptomatic relief from stuffed nose, respiratory tract congestion, bronchospasm associated with asthma, bronchitis and other similar disorders.
Class III Potassium Channel Blockers
Prolong effective refractory period by prolonging Action Potential
Treatment: ventricular tachycardia and fibrillation, conversion of atrial fibrillation or flutter to sinus rhythm, maintenance of sinus rhythm
– Amiodarone (Cordarone) – maintenance of sinus rhythm
– Bretylium (Bretylol)
– Ibutilide (Corvert)
– Dofetilide (Tykosyn)
– Sotalol (Betapace)
Amiodarone
- Has characteristics of sodium channel blockers, beta blockers, and calcium channel blockers
- Has vasodilating effects and decreases systemic vascular resistance
- Prolongs conduction in all cardiac tissue
- Decreases heart rate
- Decreases contractility of the left ventricles
Class III - Adverse Effects
- GI- Nausea vomiting and GI distress
- CNS- Weakness and dizziness
- CV-Hypotension, CHF, and arrhythmias are common.
- Amiodarone associated with potentially fatal Hepatic toxicity, ocular abnormalities and serious cardiac arrhythmias.
Drug – Drug Interactions
These drugs can cause serious toxic effects if combined with digoxin or quinidine.
Roxithromycin
It is used to treat respiratory tract, urinary and soft tissue infections. Roxithromycin is derived from erythromycin, containing the same 14-membered lactone ring. However, an N-oxime side chain is attached to the lactone ring.
Roxithromycin has similar antimicrobial spectrum as erythromycin, but is more effective against certain gram-negative bacteria, particularly Legionella pneumophilae.
When taken before a meal, roxithromycin is very rapidly absorbed, and diffused into most tissues and Phagocytes Only a small portion of roxithromycin is metabolised. Most of roxithromycin is secreted unchanged into the bile and some in expired air
Structure of the CNS
The CNS is a highly complex tissue that controls all of the body activities and serves as a processing center that links the body to the outside world.
It is an assembly of interrelated “parts”and “systems”that regulate their own and each other’s activity.
1-Brain
2-Spinal cord
The brain is formed of 3 main parts:
I. The forebrain
• cerebrum
• thalamus
• hypothalamus
II. The midbrain
III. The hindbrain
• cerebellum
• pons
• medulla oblongata
Different Parts of the Different Parts of the CNS & their functions CNS & their functions
The cerebrum(cerebral hemispheres):
It constitutes the largest division of the brain.
The outer layer of the cerebrum is known as the “cerebral cortex”.
The cerebral cortex is divided into different functional areas:
1.Motorareas(voluntary movements)
2.Sensoryareas(sensation)
3.Associationareas(higher mental activities as consciousness, memory, and behavior).
Deep in the cerebral hemispheres are located the “basal ganglia” which include the “corpus striatum”& “substantianigra”.
The basal gangliaplay an important role in the control of “motor”activities
The thalamus:
It functions as a sensory integrating center for well-being and malaise.
It receives the sensory impulses from all parts of the body and relays them to specific areas of the cerebral cortex.
The hypothalamus:
It serves as a control center for the entire autonomic nervous system.
It regulates blood pressure, body temperature, water balance, metabolism, and secretions of the anterior pituitary gland.
The mid-brain:
It serves as a “bridge”area which connects the cerebrum to the cerebellum and pons.
It is concerned with “motor coordination”.
The cerebellum:
It plays an important role in maintaining the appropriate bodyposture& equilibrium.
The pons:
It bridges the cerebellum to the medulla oblongata.
The “locus ceruleus”is one of the important areas of the pons.
The medulla oblongata:
It serves as an organ of conduction for the passage of impulses between the brain and spinal cord.
It contains important centers:
• cardioinhibitory
• vasomotor
• respiratory
• vomiting(chemoreceptor trigger zone, CTZ).
The spinal cord:
It is a cylindrical mass of nerve cells that extends from the end of the medulla oblongata to the lower lumbar vertebrae.
Impulses flow from and to the brain through descending and ascending tracts of the spinal cord.
Methyl salicylate
also known as oil of wintergreen, betula oil, methyl ester) is a natural product of many species of plants Structurally, it is methylated salicylic acid It is used as an ingredient in deep heating rubs
Antifungal
There are several classes of antifungal drugs.
The polyenes bind with sterols in the fungal cell wall, principally ergosterol. This causes the cell's contents to leak out and the cell dies. Human (and other animal) cells contain cholesterol rather than ergosterol so are much less suceptible.
Nystatin
Amphotericin B
Natamycin
The imidazole and triazole groups of antifungal drugs inhibit the enzyme cytochrome P450 14α-demethylase. This enzyme converts lanosterol to ergosterol, and is required in fungal cell wall synthesis. These drugs also block steroid synthesis in humans.
Imidazoles:
Miconazole
Ketoconazole
Clotrimazole
The triazoles are newer, and are less toxic and more effective:
Fluconazole
Itraconazole
Allylamines inhibit the enzyme squalene epoxidase, another enzyme required for ergosterol synthesis:
Terbinafine
Echinocandins inhibit the synthesis of glucan in the cell wall, probably via the enzyme 1,3-β glucan synthase:
Caspofungin
Micafungin
Others:
Flucytosine is an antimetabolite.
Griseofulvin binds to polymerized microtubules and inhibits fungal mitosis.
NSAIDs: Classification by Plasma Elimination Half Lives
Short Half Life (< 6 hours):
more rapid effect and clearance
• Aspirin (0.25-0.33 hrs),
• Diclofenac (1.1 ± 0.2 hrs)
• Ketoprofen (1.8± 0.4 hrs),
• Ibuprofen (2.1 ± 0.3 hrs)
• Indomethacin (4.6 ± 0.7 hrs)
Long Half Life (> 10 hours):
slower onset of effect and slower clearance
• Naproxen (14 ± 2 hrs)
• Sulindac (14 ± 8 hrs),
• Piroxicam (57 ± 22 hrs)