NEET MDS Lessons
Pharmacology
Phenytoin (Dilantin): for tonic-clonic and all partial seizures (not effective against absence seizures)
Mechanism: ↓ reactivation of Na channels (↑ refractory period, blocks high frequency cell firing, ↓ spread of seizure activity from focus)
Side effects: ataxia, vertigo, hirsutism (abnormal hair growth), gingival hyperplasia, osteomalacia (altered vitamin D metabolism and ↓ Ca absorption), blood dyscrasias (rare; megaloblastic anemia, etc)
Drug interactions: induces hepatic microsomal enzymes (can ↓ effectiveness of other drugs); binds tightly to plasma proteins and can displace other drugs
Streptomycin
Streptomycin was the first of a class of drugs called aminoglycosides to be discovered, and was the first antibiotic remedy for tuberculosis. It is derived from the actinobacterium Streptomyces griseus.
Streptomycin cannot be given orally, but must be administered by regular intramuscular injection.
Nimesulide
analgesic and antipyretic properties
Nimesulide is a relatively COX-2 selective, non-steroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic properties. Its approved indications are the treatment of acute pain, the symptomatic treatment of osteoarthritis and primary dysmenorrhoea in adolescents and adults above 12 years old.
Banned - not used
Biguanides
metformin
Mechanism
↓ gluconeogenesis
appears to inhibit complex 1 of respiratory chain
↑ insulin sensitivity
↑ glycolysis
↓ serum glucose levels
↓ postprandial glucose levels
Clinical use
first-line therapy in type II DM
Toxicity
no hypoglycemia
no weight gain
lactic acidosis is most serious side effect
contraindicated in renal failure
Quinolone
Quinolones and fluoroquinolones form a group of broad-spectrum antibiotics. They are derived from nalidixic acid.
Fluoroquinolone antibiotics are highly potent and considered relatively safe.
MOA : Quinolones act by inhibiting the bacterial DNA gyrase enzyme. This way they inhibit nucleic acid synthesis and act bacteriocidically.
Drugs :Nalidixic acid, Ciprofloxacin , Levofloxacin, Norfloxacin ,Ofloxacin, Moxifloxacin , Trovafloxacin
Classification
I) Esters
1. Formed from an aromatic acid and an amino alcohol.
2. Examples of ester type local anesthetics:
Procaine
Chloroprocaine
Tetracaine
Cocaine
Benzocaine- topical applications only
2) Amides
1. Formed from an aromatic amine and an amino acid.
2. Examples of amide type local anesthetics:
Articaine
Mepivacaine
Bupivacaine
Prilocaine
Etidocaine
Ropivacaine
Lidocaine
Distribution
Three major controlling factors:
Blood Flow to Tissues: rarely a limiting factor, except in cases of abscesses and tumors.
Exiting the Vascular System: Occurs at capillary beds.
- Typical Capillary Beds - drugs pass between cells
- The Blood-Brain Barrier- Tight junctions here, so drugs must pass through cells. Must then be lipid soluble, or have transport system.
- Placenta - Does not constitute an absolute barrier to passage of drugs. Lipid soluble, nonionized compounds readily pass.
- Protein Binding: Albumin is most important plasma protein in this respect. It always remains in the blood stream, so drugs that are highly protein bound are not free to leave the bloodstream. Restricts the distribution of drugs, and can be source of drug interactions.
Entering Cells: some drugs must enter cells to reach sites of action.