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.
Mechanism of Action
When a local anesthetic is injected, it is the ionized [cation] form of the local anesthetic that actually binds to anionic channel receptors in the sodium channel, thus blocking the influx of sodium ions which are responsible for lowering the -70mv resting potential towards the firing threshold of -55mv which then results in depolarization of the nerve membrane. However, only the lipid soluble nonionized [base] form of the local anesthetic can penetrate the various barriers [e.g., nerve membrane, fibrous tissue] between the site of injection and the targeted destination which is the sodium channel.
Fifth Generation:
These are extended spectrum antibiotics.
Ceftaroline, Ceftobiprole
Class IV Calcium Channel Blockers
• Block the movement of calcium into conductile and contractile myocardial cells
• Treatment: treatment of supraventricular tachycardia
– Diltiazem
– Verapamil
Adverse Effects
• Adverse effects associated with vasodilation of blood vessels throughout the body.
• CNS – dizziness, weakness, fatigue, depression and headache,
• GI upset, nausea, and vomiting.
• Hypotension CHF, shock arrhythmias, and edema
Celecoxib
is a highly selective COX-2 inhibitor and primarily inhibits this isoform of cyclooxygenase, whereas traditional NSAIDs inhibit both COX-1 and COX-2. Celecoxib is approximately 10-20 times more selective for COX-2 inhibition over COX-1.
Being a sulphonamide can cause skin rash & hypersensitivity rxn., occasional oedema& HT.
Indication
Osteoarthritis ( 100‐200mg BID ) , rheumatoid arthritis, dysmenorrhea, acute gouty attacks, acute musculoskeletal pain.
Dissociation constants
|
Local anesthetic |
pKa |
% of base(RN) at pH 7.4 |
onset of action(min) |
|
Lidocaine |
7.8 |
29 |
2-4 |
|
Bupivacaine |
8.1 |
17 |
5-8 |
|
Mepivacaine |
7.7 |
33 |
2-4 |
|
Prilocaine |
7.9 |
25 |
2-4 |
|
Articaine |
7.8 |
29 |
2-4 |
|
Procaine |
9.1 |
2 |
14-18 |
|
Benzocaine |
3.5 |
100 |
- |
Carbenicillin
Antibiotic that is chemically similar to ampicillin. Active against gram-negative germs. It is well soluble in water and acid-labile.