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Pharmacology - NEETMDS- courses
NEET MDS Lessons
Pharmacology

Mechanism of Action

When a local anesthetic is injected, it is the ionized [cation] form of the local anesthetic that actually binds to anionic channel receptors in the sodium channel, thus blocking the influx of sodium ions which are responsible for lowering the -70mv resting potential towards the firing threshold of -55mv which then results in depolarization of the nerve membrane. However, only the lipid soluble nonionized [base] form of the local anesthetic can penetrate the various barriers [e.g., nerve membrane, fibrous tissue] between the site of injection and the targeted destination which is the sodium channel.

Meperidine (Demerol)

Meperidine is a phenylpiperidine and has a number of congeners. It is mostly effective in the CNS and bowel

  • Produces analgesia, sedation, euphoria and respiratory depression.
  • Less potent than morphine, 80-100 mg meperidine equals 10 mg morphine.
  • Shorter duration of action than morphine (2-4 hrs).
  • Meperidine has greater excitatory activity than does morphine and toxicity may lead to convulsions.
  • Meperidine appears to have some atropine-like activity.
  • Does not constrict the pupils to the same extent as morphine.
  • Does not cause as much constipation as morphine.
  • Spasmogenic effect on GI and biliary tract smooth muscle is less pronounced than that produced by morphine.
  • Not an effective antitussive agent.
  • In contrast to morphine, meperidine increases the force of oxytocin-induced contractions of the uterus.
  • Often the drug of choice during delivery due to its lack of inhibitory effect on uterine contractions and its relatively short duration of action.
  • It has serotonergic activity when combined with monoamine oxidase inhibitors, which can produce serotonin toxicity (clonus, hyperreflexia, hyperthermia, and agitation)

Fluconazole: an antifungal used orally,  intravenously or vaginally to treat yeast and fungal infections. Side-effects of systemic administration include hepatotoxicity (liver damage).

  • For vaginal candidiasis (vaginal thrush), a once-only oral dose is often sufficient.

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)

DIURETICS

Specific Therapeutic Objective

Clinical State(s)

Drug(s) (Class)

Draw fluid from tissue to vascular space reduce tissue edema

Cerebral edema
glaucoma

Mannitol (Osmotic)
Glucose (Osmotic)
Glycerin (Osmotic)

Decrease renal swelling
expand tubular volume

Renal shutdown

Glucose (Osmotic)
Mannitol (Osmotic)

Modest and/or sustained decrease in venous hydrostatic pressure

Congestive heart failure
Hepatic cirrhosis
Udder edema

Hydrochlorothiazide (thiazide)
Chlorothiazide (thiazide)

Aggressive and/or short-term decrease in venous hydrostatic pressure

Congestive heart failure
Hepatic cirrhosis
Udder edema

Furosemide (loop)

Inhibit aldosterone action

Hepatic cirrhosis
Congestive heart failure

triamterene (K+ sparing)
spironolactone (K+ sparing - competitive)

Reduce potassium wasting 2o to other diuretic

Hepatic cirrhosis
Congestive heart failure

triamterene (K+ sparing)
spironolactone (K+ sparing - competitive)

Inhibit ADH action

Inappropriate ADH secretion

lithium (aquaretic)
demeclocycline (aquaretic

Increase calcium secretion

Malignant hypercalcemia

  • Paraneoplastic
  • Hypervitaminosis D

Furosemide (loop)

Reduce urine output

Diabetes insidpidus

Hydrochlorothiazide (thiazide)
Chlorothiazide (thiazide)

Urine alkalinization

Various

Carbonic anhydrase inhibitors

Carbenicillin

Antibiotic that is chemically similar to ampicillin. Active against gram-negative germs. It is well soluble in water and acid-labile.

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.
 

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