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Pharmacology - NEETMDS- courses
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Pharmacology

CLASSICATION OF ANTICOAGULANT DRUGS

1. Direct Acting Anticoagulants

a) Calcium Chelators (sodium citrate, EDTA)

b) Heparin

2. Indirect Acting Anticoagulant Drugs

a) Warfarin

Structure of the CNS 

The CNS is a highly complex tissue that controls all of the body activities and serves as a processing center that links the body to the outside world. 
It is an assembly of interrelated “parts”and “systems”that regulate their own and each other’s activity. 

1-Brain                                  
2-Spinal cord 

The brain is formed of 3 main parts: 

I. The forebrain
• cerebrum
• thalamus
• hypothalamus

II. The midbrain
III. The hindbrain
• cerebellum
• pons
• medulla oblongata

Different Parts of the Different Parts of the CNS & their functions CNS & their functions
The cerebrum(cerebral hemispheres):
It constitutes the largest division of the brain. 
The outer layer of the cerebrum is known as the “cerebral cortex”. 

The cerebral cortex is divided into different functional areas: 
1.Motorareas(voluntary movements) 
2.Sensoryareas(sensation) 
3.Associationareas(higher mental activities   as consciousness, memory, and behavior).


Deep in the cerebral hemispheres are located the “basal ganglia” which include the “corpus striatum”& “substantianigra”. 

The basal gangliaplay an important role in the control of “motor”activities

The thalamus:

It functions as a sensory integrating center for well-being and malaise. 
It receives the sensory impulses from all parts of the body and relays them to specific areas of the cerebral cortex.

The hypothalamus:

It serves as a control center for the entire autonomic nervous system. 
It regulates blood pressure, body temperature, water balance, metabolism, and secretions of the anterior pituitary gland.

The mid-brain: 

It serves as a “bridge”area which connects the cerebrum to the cerebellum and pons. 
It is concerned with “motor coordination”.

The cerebellum:

It plays an important role in maintaining the appropriate bodyposture& equilibrium.

The pons:

It bridges the cerebellum to the medulla oblongata. 
The “locus ceruleus”is one of the important areas of the pons.

The medulla oblongata:
 
It serves as an organ of conduction for the passage of impulses between the brain and spinal cord. 
It contains important centers: 
• cardioinhibitory 
• vasomotor 
• respiratory 
• vomiting(chemoreceptor trigger zone, CTZ).

The spinal cord:

It is a cylindrical mass of nerve cells that extends from the end of the medulla oblongata to the lower lumbar vertebrae. 
Impulses flow from and to the brain through descending and ascending tracts of the spinal cord.
 

Tetracycline
Tetracycline is an antibiotic produced by the streptomyces bacterium

Mechanism and Resistance Tetracycline inhibits cell growth by inhibiting translation. It binds to the 30S  ribosomal subunit and prevents the amino-acyl tRNA from binding to the A site of the ribosome. This prevents the addition of amino acids to the elongating peptide chain, preventing synthesis of proteins. The binding is reversible in nature.

Example: Chlortetracycline, oxytetracycline, demethylchlortetracycline, rolitetracycline, limecycline, clomocycline, methacycline, doxycycline, minocycline

Source: Streptomyces spp.; some are also semi-synthetic

Spectrum of activity: Broad-spectrum. Exhibits activity against a wide range of Gram-positive, Gram-negative bacteria, atypical organisms such as chlamydiae, mycoplasmas, rickettsiae and protozoan parasites.

Effect on bacteria: Bacteriostatic

Cells become resistant to tetracyline by at least two mechanisms: efflux and ribosomal protection.

Contraindications Tetracycline use should be avoided during pregnancy and in the very young (less than 6 years) because it will result in permanent staining of teeth causing an unsightly cosmetic result.

Tetracyclines also become dangerous past their expiration dates. While most prescription drugs lose potency after their expiration dates, tetracyclines are known to become toxic over time; expired tetracyclines can cause serious damage to the kidneys.

Miscellaneous: Tetracyclines have also been used for non-antibacterial purposes, having shown properties such as anti-inflammatory activity, immunosuppresion, inhibition of lipase and collagenase activity, and wound healing.

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.

Antifungal

There are several classes of antifungal drugs.

The polyenes bind with sterols in the fungal cell wall, principally ergosterol. This causes the cell's contents to leak out and the cell dies. Human (and other animal) cells contain cholesterol rather than ergosterol so are much less suceptible.

Nystatin

Amphotericin B

Natamycin

The imidazole and triazole groups of antifungal drugs inhibit the enzyme cytochrome P450 14α-demethylase. This enzyme converts lanosterol to ergosterol, and is required in fungal cell wall synthesis. These drugs also block steroid synthesis in humans.

Imidazoles:

Miconazole

Ketoconazole

Clotrimazole

 

The triazoles are newer, and are less toxic and more effective:

Fluconazole

Itraconazole

Allylamines inhibit the enzyme squalene epoxidase, another enzyme required for ergosterol synthesis:

Terbinafine

Echinocandins inhibit the synthesis of glucan in the cell wall, probably via the enzyme 1,3-β glucan synthase:

Caspofungin

Micafungin

Others:

Flucytosine is an antimetabolite.

Griseofulvin binds to polymerized microtubules and inhibits fungal mitosis.

 

Ketoconazole

synthetic antifungal drug

used for infections such as  athlete's foot, ringworm, candidiasis (yeast infection or thrush), jock itch.

Ketoconazole is used to treat eumycetoma, the fungal form of mycetoma.

MOA: Ketoconazole is imidazole structured, and interferes with the fungal synthesis of  ergosterol, the main constituent of cell membranes, as well as certain enzymes. It is specific for fungi, as mammalian cell membranes contain no ergosterol.

Sensitive fungi Ketoconazole inhibits growth of  dermatophytes and  yeast species (such as Candida albicans).

ANTIDEPRESSANTS

Monoamine uptake inhibitors

1. Tricyclic antidepressants (TCAs)
2. Selective serotonin reuptake inhibitors (SSRIs)
3. Serotonin-norepinephrine reuptake inhibitors(SNRIs)
4. Norepinephrine reuptake inhibitor

Monoamine oxidase inhibitors (MAOIs) 

Monoamine receptor antagonists 

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