NEET MDS Lessons
Pharmacology
Gastric acid neutralizers (antacids)
Antacids act primarily in the stomach and are used to prevent and treat peptic ulcer. They are also used in the treatment of Reflux esophagitis and Gastritis.
Mechanism of action:
Antacids are alkaline substances (weak bases) that neutralize gastric acid (hydrochloric acid) they react with hydrochloric acid in the stomach to produce neutral or less acidic or poorly absorbed products and raise the pH of stomach secretion.
Antacids are divided into systemic and non-systemic.
• Systemic antacids (e.g. sodium bicarbonate) are highly absorbed into systemic circulation and enter body fluids. Therefore, they may alter acid–base balance. They can be used in the treatment of metabolic acidosis.
Non-systemic: they do not alter acid–base balance significantly, because they are not well-absorbed into the systemic circulation. They are used as gastric antacids; and include:
• Magnesium compounds such as magnesium hydroxide and magnesium sulphate MgS2O3. They have relatively high neutralizing capacity, rapid onset of action, however, they may cause diarrhoea and hypermagnesemia.
• Aluminium compounds such as aluminium hydroxide. Generally, these have low neutralizing capacity, slow onset of action but long duration of action. They may cause constipation.
• Calcium compounds such as. These are highly effective and have a rapid onset of action but may cause hypersecretion of acid (acid - rebound) and milk-alkali syndrome (hence rarely used in peptic ulcer disease).
Therefore, the most commonly used antacids are mixtures of aluminium hydroxide and magnesium hydroxide .
Seizure classification:
based on degree of CNS involvement, involves simple ( Jacksonian; sensory or motor cortex) or complex symptoms (involves temporal lobe)
1. Generalized (whole brain involved):
a. Tonic-clonic:
Grand Mal; ~30% incidence; unconsiousness, tonic contractions (sustained contraction of muscle groups) followed by clonic contractions (alternating contraction/relaxation); happens for ~ 2-3 minutes and people don’t breathe during this time
Drugs: phenytoin, carbamazepine, Phenobarbital, lamotrigine, valproic acid
Status epilepticus: continuous seizures; use diazepam (short duration) or diazepam + phenytoin
b. Absence:
Petit Mal; common in children; frequent, brief lapses of consciousness with or without clonic motor activity; see spike and wave EEg at 3 Hz (probably relates to thalamocorticoreverburating circuit)
Drugs: ethosuximide, lamotrigine, valproic acid
c. Myoclonic: uncommon; isolated clinic jerks associated with bursts of EEG spikes;
Drugs: lamotrigine, valproic acid
d. Atonic/akinetic: drop seizures; uncommon; sudden, brief loss of postural muscle tone
Drugs: valproic acid and lamotrigine
2. Partial: focal
a. Simple: Jacksonian; remain conscious; involves motor or sensory seizures (hot, cold, tingling common)
Drugs: carbamazepine, phenytoin, Phenobarbital, lamotrigine, valproic acid, gabapentin
b. Complex: temporal lobe or psychomotor; produced by abnormal electrical activity in temporal lobe (involves emotional functions)
Symptoms: abnormal psychic, cognitive, and behavioral function; seizures consist of confused/altered behavior with impaired consciousness (may be confused with psychoses like schizophrenia or dementia)
Drugs: carbamazepine, phenytoin, laotrigine, valproic acid, gabapentin
Generalizations: most seizures can’t be cured but can be controlled by regular administration of anticonvulsants (many types require treatment for years to decades); drug treatment can effectively control seizures in ~ 80% of patients
Opiate Antagonists
Opiate antagonists have no agonist properties. They are utilized to reverse opiate induced respiratory depression and to prevent drug abuse.
A. Naloxone
Pure opiate antagonist , Short duration of action, Only 1/50th as potent orally as parenterally
B. Naltrexone
Pure opiate antagonist, Long duration of action, Better oral efficacy
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
Topical Anesthetics
Benzocaine
Benzocaine is a derivative of procaine, an ester type local anesthetic, and is poorly soluble in water and is
available only as a topical anesthetic.
- Localized allergic reactions are sometimes encountered
- Overdosing is unlikely as benzocaine is poorly absorbed into the blood, which decreases the likelihood of systemic toxicity.
- The onset of surface anesthesia is rapid requiring less than one minute.
Tetracaine
- Tetracaine is an ester type local anesthetic
- Topically applied tetracaine as opposed to benzocaine has a prolonged duration of action.
Cocaine
- Cocaine is a ester type anesthetic that is used exclusively as a topical agent.
- Cocaine is unique among topical and injectable anesthetics in that it has vasoconstrictive as well as anesthetic properties. It is used sparingly because of its abuse potential but is still used when hemostasis of mucous membranes is essential.
- Cocaine is generally available in concentrations of 2-10 % solution.
Lidocaine
- Lidocaine is an amide local anesthetic that is available in injectable and topical formulations.
- It is available in gel, viscous solution, ointment and aerosol preparations in concentrations ranging from 2-10 %.
- The onset of anesthesia is slower relative to benzocaine but, the duration is about the same.
- Absorption into the bloodstream is greater than benzocaine providing a greater risk of systemic toxicity.
Methods of general anesthesia
CIRCLE SYSTEM
*HIGH-FLOW
FRESH GAS FLOW > 3 l/min.
*LOW-FLOW
FGF ok. 1l/min.
*MINIMAL-FLOW
FGF ok. 0,5 l/min.
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