NEET MDS Lessons
Pharmacology
Amoxicillin
a moderate-spectrum
β-lactam antibiotic used to treat bacterial infections caused by susceptible
Mode of action Amoxicillin acts by inhibiting the synthesis of bacterial cell walls. It inhibits cross-linkage between the linear peptidoglycan polymer chains that make up a major component of the cell wall of Gram-positive bacteria. microorganisms. It is usually the drug of choice within the class because it is better absorbed, following oral administration, than other beta-lactam antibiotics. Amoxicillin is susceptible to degradation by β-lactamase-producing bacteria, and so is often given clavulanic acid.
Microbiology Amoxicillin is a moderate-spectrum antibiotic active against a wide range of Gram-positive, and a limited range of Gram-negative organisms
Susceptible Gram-positive organisms : Streptococcus spp., Diplococcus pneumoniae, non β-lactamase-producing Staphylococcus spp., and Streptococcus faecalis.
Susceptible Gram-negative organisms Haemophilus influenzae, Neisseria gonorrhoeae, Neisseria meningitidis, Escherichia coli, Proteus mirabilis and Salmonella spp.
Resistant organisms Penicillinase producing organisms, particularly penicillinase producing Staphylococcus spp. Penicillinase-producing N. gonorrhoeae and H. influenzae are also resistant
All strains of Pseudomonas spp., Klebsiella spp., Enterobacter spp., indole-positive
Proteus spp., Serratia marcescens, and Citrobacter spp. are resistant.
The incidence of β-lactamase-producing resistant organisms, including E. coli, appears to be increasing.
Amoxicillin and Clavulanic acid Amoxicillin is sometimes combined with clavulanic acid, a β-lactamase inhibitor, to increase the spectrum of action against
Gram-negative organisms, and to overcome bacterial antibiotic resistance mediated through β-lactamase production.
COAGULANTS
An agent that produces coagulation (Coagulation is a complex process by which blood forms clots).
ANTICOAGULANTS
An anticoagulant is a substance that prevents coagulation; that is, it stops blood from clotting.
Anticoagulants:
Calcium Chelators (sodium citrate, EDTA)
Heparin
Dalteparin Sodium (Fragmin) -Low molecular-weight heparin
Enoxaparin - Low molecular-weight heparin
Tinzaparin Sodium - Low molecular-weight heparin
Warfarin
Lepirudin - recombinant form of the natural anticoagulant hirudin: potent and specific Thrombin inhibitor
Bivalirudin - analog of hirudin: potent and specific Thrombin inhibitor
Procoagulants:
Desmopressin acetate
Antiplatelet Drugs:
Acetylsalicylic Acid, Ticlopidine, Sulfinpyrazone, Abciximab , Clopidogrel bisulfate
Fibrinolytic Drugs:
Tissue Plasminogen Activator (t-PA, Activase), Streptokinase (Streptase),
Anistreplase, Urokinase
Antagonists:
Protamine sulfate, Aminocaproic acid
Pharmacological agents used to treat blood coagulation disorders fall in to three major categories:
1. Anticoagulants: Substances that prevent the synthesis of a fibrin network which inhibits coagulation and the formation of arterial thrombi and thromboembolic clots.
2. Antiplatelet agents: Substances that reduce the adhesion and aggregation of platelets.
3. Fibrinolytic agents: Substances that promote the destruction of already formed blood clots or thrombi by disrupting the fibrin mesh.
Etomidate -Intravenous Anesthetics
- A nonbarbiturate anesthetic used primarily to induce surgical anesthesia.
- It does not produce analgesia.
- Etomidate has minimal effect on the cardiovascular system and respiration during induction of anesthesia.
- Like the barbiturates, etomidate decreases cerebral blood flow, cerebral metabolic rate and intracranial pressure.
- No changes in hepatic, renal or hematologic function have been reported.
- Myoclonic muscle movements are relatively common.
- Postoperative nausea and vomiting are more common with etomidate than with barbiturates.
Gabapentin (Neurontin): newer; for generalized tonic-clonic seizures and partial seizures (partial and complex)
Mechanism: unknown but know doesn’t mimic GABA inhibition or block Ca currents
Side effects: dizziness, ataxia, fatigue; drug well-tolerated and no significant drug interactions
Aspirin
Mechanism of Action
ASA covalently and irreversibly modifies both COX-1 and COX-2 by acetylating serine-530 in the active site Acetylation results in a steric block, preventing arachidonic acid from binding
Uses of Aspirin
Dose-Dependent Effects:
Low: < 300mg blocks platelet aggregation
Intermediate: 300-2400mg/day antipyretic and analgesic effects
High: 2400-4000mg/day anti-inflammatory effects
Often used as an analgesic (against minor pains and aches), antipyretic (against fever), and anti-inflammatory. It has also an anticoagulant (blood thinning) effect and is used in long-term low-doses to prevent heart attacks
Low-dose long-term aspirin irreversibly blocks formation of thromboxane A2 in platelets, producing an inhibitory affect on platelet aggregation, and this blood thinning property makes it useful for reducing the incidence of heart attacks
Its primary undesirable side effects, especially in stronger doses, are gastrointestinal distress (including ulcers and stomach bleeding) and tinnitus. Another side effect, due to its anticoagulant properties, is increased bleeding in menstruating women.
Itraconazole:
The drug may be given orally or intravenously.
Ampicillin offered a broader spectrum of activity than either of the original penicillins and allowed doctors to treat a broader range of both Gram-positive and Gram-negative infections. Ampicillin is often used in molecular biology as a test for the uptake of genes (e.g., by plasmids) by bacteria (e.g., E. coli)