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Pharmacology - NEETMDS- courses
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Pharmacology

Loperamide

  • Similar chemically and pharmacologically to Diphenoxylate.
  • Slows gastrointestinal motility by effects on the circular and longitudinal muscles of the intestine.
  • Not well absorbed following oral administration.
  • Useful in the treatment of diarrhea.

Osmotic diuretics

An osmotic diuretic is a type of diuretic that inhibits reabsorption of water and sodium. They are pharmacologically inert substances that are given intravenously. They increase the osmolarity of blood and renal filtrate.

Mechanism(s) of Action

1.    Reduce tissue fluid (edema) 
2.    Reflex cardiovascular effect by osmotic retention of fluid within vascular space which increases blood volume (contraindicated with Congestive heart failure) 
3.    Diuretic effect

o    Makes H2O reabsorption far more difficult for tubular segments insufficient Na & H2O capacity in distal segments
o    Increased intramedullary blood flow (washout)
o    Incomplete sodium recapture (asc. loop). this is indirect inhibition of Na reabsorption (Na stays in tubule because water stays) 
o    Net diuretic effect: 
    Tubular concentration of sodium decreases 
    Total amount of sodium lost amount increases 
    GFR unchanged or slightly increased

Toxicity

Circulatory overload, dilutional hyponatremia,  Hyperkalemia, edema, skin necrosis

Agents
Mannitol

Properties of inhalation anesthetics

The lower the solubility, the faster the onset and the faster the recoverability.

All general anesthetics:

1. inhibit the brain from responding to sensory stimulation.

2. block the sensory impulses from being recorded in memory.

3. prevent the sensory impulses from evoking “affect”.

Most general anesthetic agents act in part by interacting with the neuronal membranes to affect ion channels and membrane excitability.

· If the concentration given is too low:

1. Movement may occur

2. Reflex activity present (laryngeal spasm)

3. Hypertension

4. Awareness

Premedication of analgesic drugs and muscle relaxants are designed to minimise these effects

· If the concentration given is too high:

1. Myocardial depression

2. Respiratory depression

3. Delayed recovery

Lamotrigine (Lamictal): newer; broad spectrum (for most seizure types)

Mechanism: ↓ reactivation of Na channels (↑ refractory period, blocks high frequency cell firing)

Side effects: dizziness, ataxia, fatigue, nausea, no significant drug interactions

Inhalational Anesthetics

The depth of general anesthesia is directly proportional to the partial pressure of the anesthetic agent in the brain. These agents enter the body through the lungs, dissolve in alveolar blood and are transported to the brain and other tissues.

A. Rate of induction and rate of recovery from anesthesia:

1. The more soluble the agent is in blood, the more drug it takes to saturate the blood and the more time it takes to raise the partial pressure and the depth of anesthesia.

2. The less soluble the agent is in blood, the less drug it takes to saturate the blood and the less time it takes to raise the partial pressure and depth of anesthesia.

 

B. MAC (minimum alveolar concentration)

The MAC is the concentration of the anesthetic agent that represents the ED50 for these agents. It is the alveolar concentration in which 50% of the patients will respond to a surgical incision.

The lower the MAC the more potent the general anesthetic agent.

C. Inhalation Anesthetic Agents 

  • Nitrous Oxide
  • Ether
  • Halothane
  • Enflurane
  • Isoflurane

Pharmacology is the study of drugs and the way they interact with living systems.  Clinical pharmacology is the study of drugs in humans.

A drug is any chemical that can effect living processes.

Therapeutics: the medical use of drugs.

An ideal drug has several important properties.  Three of these properties are of utmost importance: effectiveness, safety and selectivity. 

Effectiveness: This is the most important quality that a drug can have.  Effectiveness refers to the drug's ability to do what it is supposed to do.

Safety:  Although no drug can be totally safe, proper usage can lessen the risks of adverse effects.

Selectivity:  A truly selective drug would have no side effects, and would effect only the body process' for which it is designed and given.  Therefore, there is no such thing as a selective drug.

Pharmacokinetics: The way the body deals with a drug.  Pharmacokinetics is concerned with the processes of absorption, distribution, metabolism and excretion.

Pharmacodynamics:  What a drug does to the body.

Pharmacokinetics and pharmacodynamics are two of the processes that determine how a person will respond to a drug.  Other factors include how a drug is administered (dose, route, and timing of administration), interactions with other drugs, and individual physiological variables (weight, age, function of body systems).

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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