NEET MDS Lessons
Pharmacology
First Generation Cephalosporins
Prototype Drugs are CEFAZOLIN (for IV use) and CEPHALEXIN (oral use).
1. Staph. aureus - excellent activity against b-lactamase-producing strains
Not effective against methicillin-resistant Staph. aureus & epidermidis
2. Streptococci - excellent activity versus Streptococcus sp.
Not effective against penicillin-resistant Strep. pneumoniae
3. Other Gm + bacteria - excellent activity except for Enterococcus sp.
4. Moderate activity against gram negative bacteria.
Caution: resistance may occur in all cases.
Susceptible organisms include:
E. coli
Proteus mirabilis
Indole + Proteus sp. (many strains resistant)
Haemophilus influenzae (some strains resistant)
Neisseria sp. (some gonococci resistant)
Uses
1. Upper respiratory tract infections due to Staph. and Strep.
2. Lower respiratory tract infections due to susceptible bacteria e.g. Strep.pneumoniae in penicillin-allergic patient (previous rash)
3. Uncomplicated urinary tract infections (Cephalexin)
4. Surgical prophylaxis for orthopedic and cardiovascular operations (cefazolin preferred because of longer half-life)
5. Staphylococcal infections of skin and skin structure
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
Antidiarrheal
Antidiarrheal drugs may be given to relieve the symptom (non-specific therapy) or may be given to treat the underlying cause of the symptom (specific therapy).
Ι. Drugs used for the symptomatic (non-specific) treatment of diarrhoea include:
• Opiates and opiate derivatives are the most effective (such as morphine), but it is not used because of potentially serious adverse effects. Other agents, such as diphenoxylate and loperamide, are commonly used.
• Adsorbent – demulcent products such as kaolin – pectin preparation may be included in antidiarrheal preparations. Unfortunately, they may adsorb nutrients and other drugs, including the antidiarrheal agents if given concurrently.
• Anticholinergic agents e.g. atropine is occasionally used to decrease abdominal cramping and pain associated with diarrhoea.
ΙΙ. Specific therapy may include the use of antibacterial agents that are recommended for use in carefully selected cases of bacterial enteritis. For example, severe diarrhoea by salmonella, shigella, campylobacter and clostridia species can be treated by antibiotics (ampicillin, chloramphenicol, co-trimoxazole).
Heparin:
- Inhibits blood coagulation by forming complexes with an α2-globulin (Antithrombin III) and each of the activated proteases of the coagulation cascade (Kallikrein, XIIa, XIa, IXa, Xa, and Thrombin). After formation of the heparin-ATIII-coagulation factor, heparin is released and becomes available again to bind to free ATIII.
- Blocks conversion of Prothrombin to Thrombin and thus inhibits the synthesis of Fibrin from Fibrinogen.
- Inhibits platelet function and increases vascular permeability. May induce moderate to severe thrombocytopenia.
- Is prescribed on a “unit” basis.
- Heparin is not effective after oral administration and is generally administered by intravenous or subcutaneous injection. Intramuscular injections should be avoided.
- Heparin does not cross the placenta and does not pass into the maternal milk.
- is contraindicated in any situation where active bleeding must be avoided.
Ulcerative lesions, intracranial hemorrhage, etc.
Overdosage:
• Simple withdrawal.
• Protamine sulfate: Highly basic peptide that binds heparin and thus neutralizes its effects.
Dextromethorphan
O-methylated dextrorphan, Excellent oral antitussive, No analgesic effect, No GI effects, No respiratory depression
EPHEDRINE
It act indirectly and directly on α and β receptors. It increases blood pressure both by peripheral vasoconstriction and by increasing the cardiac output. Ephedrine also relaxes the bronchial smooth muscles.
Ephedrine stimulates CNS and produces restlessness, insomnia, anxiety and tremors.
Ephedrine produces mydriasis on local as well as systemic administration.
Ephedrine is useful for the treatment of chronic and moderate type of bronchial asthma, used as nasal decongestant and as a mydriatic without cycloplegia. It is also useful in preventing ventricular asystole in Stokes Adams syndrome.
PHARMACOLOGY OF LOCAL ANESTHETICS
Characteristics
1. Block axon conduction (nerve impulse) when applied locally in appropriate concentrations.
2. Local anesthetic action must be completely reversible; however, the duration of the anesthetic block should be of sufficient length to allow completion of the planned treatment.
3. Produce minimal local toxic effects such as nerve and muscle damage as well as minimal systemic toxic effects of organ systems such as the cardiovascular and central nervous system.