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Pharmacology - NEETMDS- courses
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Pharmacology

SULPHONAMIDES

Derivative of  sulphonilamide (Para-amino Benzene (PABA ) sulphonamide).

Anti-bacterial spectrum

Bacteriostatic to gram + and gram - bacteria. but bactericidal concentrations arce attained in urine. S pyogencs. H influenzae.E coli, few- Staph aureus. gonococci. pneumococci, proteus, shigella and Lymphogranuloma venereum.

Mechanism of action

Inhibits bacterial folate synthetase as they compete with PABA

Less soluble in acid urine and may precipitate to cause crystalluria.

Accumulate in patients with renal failure and can cause toxicity

Classification

Shart Acting (4-8 Hrs) sulphadiazine, sulphamethizole.

Intermediate acting(8-16 Hrs): sulphamethoxazole , sulphaphenazole

Long Acting(l-7days): sulphamethoxypyridazine.

Ultralong Acting(3-8days): sulfaline

Adverse effects

I. nausea, vomiting and epigastric pain

2. crystalluria

3. hypersensitivity-like polyarthritis nodosa. Steven-Johnson Syndrome. photosenstivity

4.hemolysis in G-6PD deficiency

5. kernicterus

They inhibit metabolism of phenytoin. tolbutamide. methotrexate

Therapeutic Use

UTI Meningitis, Streptococcal pharyngitis, Bacillary Dysentery

Drugs Used in Diabetes

Goals of diabetes treatment

lower serum glucose to physiologic range
keep insulin levels in physiologic range
eliminate insulin resistance

best initial step in management: weight loss, contractile-based exercise weight loss is more important for insulin sensitivity than is a low-carb diet

Modalities of diabetes treatment

Type I DM

insulin
low-sugar diet

Type II DM
exercise
diet
insulin

6 classes of drugs 

Insulin
Sulfonylureas -    Glyburide
Meglitinides  - Nateglinide
Biguanides    Metformin    
Glitazones (thiazolidinediones)    Pioglitazone
α-glucosidase inhibitors    Acarbose
GLP-1 mimetics (incretin mimetics)    Exenatide
Amylin analog    Pramlintide

Kinins
Peptide that are mediated in the inflammation.
Action of kinin:
On CVS: vasodilatation in the kidneys, heart, intestine, skin, and liver. It is 10 times active than histamine as vasodilator.

On exocrine and endocrine glands: kinin modulate the tone of pancreas and salivery glands and help regulate GIT motility, also affect the transport of water and electrolytes, glucose and amino acids through epithelial cell transport.

TRIMETHOPRIM

It is a diaminopyrimidine. It inhibits bacterial dihydrofolate reductase( DHFRase).

In combination with sulphamethoxzole it is called Co-trimoxazole.

Spectrum of action

 S. Typhi. Serratia. Klebsiela and many sulphonamide resistant strains of Staph.aureus. Strep pyogens

Adverse effects

Megaloblastic anemia. i.e.. due to folate defeciency.

Contraindicated in pregnancy.

Diuretics if given with co-trimoxazole cause thrombocytopenia.

Uses

I. UTI. 2. RTI. 3. Typhoid. 5. Septicemias. 5. Whooping cough

 

BradyKinin

An endogenous vasodilator occurring in blood vessel walls. 
At least two distinct receptor types, B1 and B2, appear to exist for BradyKinin

Roles of bradykinin:

1) Mediator of inflammation and pain.
2) Regulation of microcirculation.
3) Their production is interrelated with clotting and fibrinolysin systems.
4) Responsible for circulatory change after birth.
5) Involved in shock and some immune reactions.

Class IV Calcium Channel Blockers
• Block the movement of calcium into conductile and contractile myocardial cells 
• Treatment: treatment of supraventricular tachycardia 
– Diltiazem 
– Verapamil 

Adverse Effects 
• Adverse effects associated with vasodilation of blood vessels throughout the body. 
• CNS – dizziness, weakness, fatigue, depression and headache, 
• GI upset, nausea, and vomiting. 
• Hypotension CHF, shock arrhythmias, and edema 
 

Stimulants: 

Amphetamines: amphetamine is a substrate of serotonin and NE uptake transporters so in cytoplasm, it competes for transport into storage vesicles → ↑ [ ] in cytoplasm then excess amines bind to membrane transporter and are transported out of cell

Drugs: 
a.    Dextroamphetamine: psychomotor stimulant (↓ fatigue), short-term weight loss, prevents narcolepsy
b.    Methylphenidate (Ritalin): prevents narcolepsy, treatment for ADD and ADHD
c.    Methamphetamine: psychomotor stimulant, abused widely (cheap, easy to make)

Side effects: 
a.    CNS: euphoria, anxiety, agitation, delirium, paranoia, panic, suicidal/homicidal impulses, psychoses, tolerance (develops rapidly to most CNS effects), physical dependence (not clinically relevant)
b.    CV: headache, chills, arrhythmias and HTN (may be fatal)

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