Chloral hydrate

1. Short-acting sleep inducer—less risk of “hangover” effect the next day.
2. Little change on REM sleep.
3. Metabolized to trichloroethanol, an active metabolite; further metabolism inactivates the drug.
4. Used for conscious sedation in dentistry.
5. Can result in serious toxicity if the dose is not controlled.

Carbonic anhydrase inhibitors

Acetazolamide, Dichlorphenamide, Methazolamide, Ethoxzolamide

Mechanism of Action

1.    Carbonic anhydrase (CA) facilitates excretion of H+ and recovery of bicarbonate by the proximal renal tubule and ciliary epithelium of the eye. Sodium is recovered in exchange for H+. 
2.    Inhibitors block CA block sodium recovery. A very mild diuresis is produced (this is really a side effect of their use in glaucoma) because relatively unimportant mechanism for Na recovery and because proximal tubule site means that other sodium recovery mechansims continue to process their normal fraction of the sodium load.
 

Classification Based on

a. Chemical structure

I. Sulphonamidcs.and others - c.g.. sulphadiazine. etc.

2. Beta-lactum ring - e.g.. penicillin

3. Tetracycline - e.g.. Oxytetracycline,.doxycycline.etc.

b. Mechanism of action

1. Inhibits cell-wall synthesis - penicillin. cephalosporin..cycloserine. etc.

2. Cause leakage from cell-membrane – polypeptides (polymyxin,  Bacitracin), polyenes (Nystatin)

3. Inhibit protein synthesis - tetracyclines. chloramphenicols. erythromycin.

4. Cause mis-reading of mRNA code - aminoglycosides

5. Interfere with DNA function - refampicin.. metronidazole

6. Interfere with intermediary metabolism - sulphonamides. ethambutole

c. Type of organism against which it is primarily activate

I. Antibacterial - penicillin.

2. Antifungal - nystatin.

d. Spectrum of activity

1. Broad spectrum - tetracylines .

2. Narrow spectrum - penicillin G (penG). streptomycin.erythromycin

e. Type of action

I. Bacteriostatic - sulphonamides, erythromycin.tertracyclines

2. Bacteriocidal - penicillin. aminoglycoside

f. Source

I. Fungi - penicillin. cephalosporins

2. Bacteria - Polymyxin B

Griseofulvin

• Griseofulvin is an antifungal drug. It is used both in animals and in humans, to treat ringworm infections of the skin and nails. It is derived from the mold Penicillium griseofulvum.
• It is administered orally.

Benzodiazepines
All metabolites are active sedatives except the final glucuronide product. Elimination half-life varies a great deal from drug to drug.

?-Hydroxylation is a rapid route of metabolism that is unique to triazolam, midazolam, and alprazolam.
This accounts for the very rapid metabolism and short sedative actions of these drugs.

Pharmacological effects of benzodiazepines

- Antianxiety.
- Sedation.
- Anticonvulsant (including drug-induced convulsions).
- Amnesia, especially drugs like triazolam.
- Relax skeletal muscle (act on CNS polysynaptic pathways).

Indications

- IV sedation, (e.g., midazolam, diazepam, lorazepam).
- Antianxiety.
- Sleep induction.
- Anticonvulsant (e.g., diazepam, clonazepam).
- Panic disorders.
- Muscle relaxation.


Adverse effects

- Ataxia, confusion.
- Excessive sedation.
- Amnesia (not a desired effect with daytime sedation).
- Altered sleep patterns (increase stage 2 and decrease stage 4 sleep).

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.