Sedative-Hypnotic Drugs

Sedative drug is the drug that reduce anxiety (anxiolytic) and produce sedation and referred to as minor tranquillisers. 

Hypnotic drug is the drug that induce sleep

Effects: make you sleepy; general CNS depressants

Uses: sedative-hypnotic (insomnia ), anxiolytic (anxiety, panic, obsessive compulsive, phobias), muscle relaxant (spasticity, dystonias), anticonvulsant (absence, status epilepticus, generalized seizures—rapid tolerance develops), others (pre-operative medication and endoscopic procedures,  withdrawal from chronic use of ethanol or other CNS depressants)

1- For panic disorder alprazolam is effective.

2- muscle disorder: (reduction of muscle tone and coordination) diazepam is useful in treatment of skeletal muscle spasm e.g. muscle strain and spasticity of degenerative muscle diseases.

3-epilepsy: by increasing seizure threshold.

Clonazepam is useful in chronic treatment of epilepsy while diazepam is drug of choice in status epilepticus.

4-sleep disorder: Three BDZs are effective hypnotic agents; long acting flurazepam, intermediate acting temazepam and short
acting triazolam. They decrease the time taken to get to sleep They increase the total duration of sleep

5-control of alcohol withdrawals symptoms include diazepam, chlordiazepoxide, clorazepate and oxazepam.

6-in anesthesia: as preanesthetic amnesic agent (also in cardioversion) and as a component of balanced anesthesia

Flurazepam significantly reduce both sleep induction time and numbers of awakenings and increase duration of sleep and little rebound insomnia. It may cause daytime sedation.

Temazepam useful in patients who experience frequent awakening, peak sedative effect occur 2-3 hr. after an oral dose.

Triazolam used to induce sleep in recurring insomnia and in individuals have difficulty in going to sleep, tolerance develop within few days and withdrawals result in rebound insomnia therefore the drug used intermittently.

Drugs and their actions

1. Benzodiazepines: enhance the effect of gamma aminobutyric acid (GABA) at GABA receptors on chloride channels. This increases chloride channel conductance in the brain (GABA A A receptors are ion channel receptors).

2. Barbiturates: enhance the effect of GABA on the chloride channel but also increase chloride channel conductance independently of GABA, especially at high doses 

3. Zolpidem and zaleplon: work in a similar manner to benzodiazepines but do so only at the benzodiazepine (BZ1) receptor type. (Both BZ1and BZ2 are located on chloride channels.)

4. Chloral hydrate: probably similar action to barbiturates.

5. Buspirone: partial agonist at a specific serotonin receptor (5-HT1A).

6. Other sedatives (e.g., mephenesin, meprobamate, methocarbamol, carisoprodol, cyclobenzaprine): 
mechanisms not well-described. Several mechanisms may be involved.

7. Baclofen: stimulates GABA linked to the G protein, Gi , resulting in an increase in K + conductance and a decrease in Ca²⁺ conductance. (Other drugs mentioned above do not bind to the GABA B receptor.) 

8. Antihistamines (e.g., diphenhydramine): block H1 histamine receptors. Doing so in the CNS leads to sedation.

9. Ethyl alcohol: its several actions include a likely effect on the chloride channel.

Erythromycin

used for people who have an allergy to penicillins. For respiratory tract infections, it has better coverage of atypical organisms, including  mycoplasma. It is also used to treat outbreaks of chlamydia, syphilis, and gonorrhea.

Erythromycin is produced from a strain of the actinomyces Saccaropolyspora erythraea, formerly known as Streptomyces erythraeus.

ANTIBIOTICS

Chemotherapy: Drugs which inhibit or kill the infecting organism and have no/minimum effect on the recipient.

Antibiotic these are substances produced by microorganisms which suppress the growth of or kill other micro-organisms at very low concentrations.

Anti-microbial Agents: synthetic as well as naturally obtained drugs that attenuate micro-organism.

SYNTHETIC ORGANIC ANTIMICROBIAL DRUGS

Sulfonamides

Trimethoprim-sulfamethoxazole

Quinolones – Ciprofloxacin

ANTIBIOTICS THAT ACT ON THE BACTERIAL CELL WALL

Penicillins

Cephalosporins

Vancomycin

INHIBITORS OF BACTERIAL PROTEIN SYNTHESIS

Aminoglycosides - Gentamicin

Antitubercular Drugs: Isoniazid & Rifampin

Tetracyclines

Chloramphenicol

Macrolides – Erythromycin, Azithromycin

Clindamycin

Mupirocin

Linezolid

 ANTIFUNGAL DRUGS

Polyene Antibiotics (Amphotericin B, Nystatin and Candicidin)

Imidazole and Triazole Antifungal Drugs

Flucytosine

Griseofulvin

ANTIPROTOZOAL DRUGS

Antimalarial Drugs – Quinine, Chloroquine, Primaquine

Other Antiprotozoal Drugs – Metronidazole, Diloxanide, Iodoquinol

 ANTIHELMINTHIC DRUGS

Praziquantel

Mebendazole

Ivermectin

ANTIVIRAL DRUGS

Acyclovir

Ribavirin

Dideoxynucleosides

Protease inhibitors

Antianginal Drugs

Organic Nitrates :
Short acting: Glyceryl trinitrate (Nitroglycerine, GTN), Amyl Nitrate
Long Acting: Isosrbide dinitrate (Short acting by sublingual route), Erythrityl tetranitrate, penta erythrityl tetranitrate

Beta-adrenergic blocking agents : Propanolol, Metoprolol
Calcium channel blockers Verapamil, Nifedipine, Dipyridamole
 
Mechanism of action 
– Decrease myocardial demand 
– increase blood supply to the myocardium

Doxycycline

Commonly prescribed for infections and to treat acne. treat urinary tract infections, gum disease, and other bacterial infections such as gonorrhea and chlamydia., as a prophylactic treatment for infection by Bacillus anthracis (anthrax). It is also effective against Yersinia pestis and malaria.

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.