NEET MDS Lessons
Pharmacology
Acid-Peptic disorders
This group of diseases include peptic ulcer, gastroesophageal reflux and Zollinger-Ellison syndrome.
Pathophysiology of acid-peptic disorders
Peptic ulcer disease is thought to result from an imbalance between cell– destructive effects of hydrochloric acid and pepsin on the one side, and cell-protective effects of mucus and bicarbonate on the other side. Pepsin is a proteolytic enzyme activated in gastric acid (above pH of 4, pepsin is inactive); also it can digest the stomach wall. A bacterium, Helicobacter pylori, is now accepted to be involved in the pathogenesis of peptic ulcer.
In gastroesophageal reflux the acidic contents of the stomach enter into the oesophagus causing a burning sensation in the region of the heart; hence the common name heartburn or other names such as indigestion and dyspepsia.
However, Zollinger-Ellison syndrome is caused by a tumor of gastrin secreting cells of the pancreas characterized by excessive secretion of gastrin that stimulates gastric acid secretion.
These disorders can be treated by the following classes of drugs:
A. Gastric acid neutralizers (antacids)
B. Gastric acid secretion inhibitors (antisecretory drugs)
C. Mucosal protective agents
D. Drugs that exert antimicrobial action against H.pylori
Class II Beta Blockers
Block SNS stimulation of beta receptors in the heart and decreasing risks of ventricular fibrillation
– Blockage of SA and ectopic pacemakers: decreases automaticity
– Blockage of AV increases the refractory period
- Increase AV nodal conduction ´
- Increase PR interval
- Reduce adrenergic activity
Treatment: Supraventricular tachycardia (AF, flutter, paroxysmal supraventricular tachycardia
– Acebutolol
– Esmolol
– Propanolol
Contraindications and Cautions
• Contraindicated in sinus bradycardia P < 45
• Cardiogenic shock, asthma or respiratory depression which could be made worse by the blocking of Beta receptors.
• Use cautiously in patients with diabetes and thyroid dysfunction, which could be altered by the blockade of Beta receptors
• Renal and hepatic dysfunction could alter the metabolism and excretion of these drugs.
Estimation of the risk of anesthesia (American Society of Anesthesiologists scale)
• ASA 1: healthy patient.
• ASA 2: patient with stable, treated illness like arterial hypertension, diabetes melitus, asthma bronchiale, obesity
• ASA 3: patient with systemic illness decreasing sufficiency like heart illness, late infarct
• ASA 4: patient with serious illness influencing his state like renal insuficiency, unstable hypertension, circulatory insuficiency
• ASA 5: patient in life treatening illness
• ASA 6: brain death- potential organ donor
Codeine
Codeine is methyl morphine, with a methyl substitution on the phenolic hydroxyl group of morphine. It is more lipophilic than morphine and thus crosses the blood–brain barrier faster.
- classified as a simple, or mild analgesic, codeine is often used in low doses as an oral analgesic has a much better oral/parenteral absorption ratio than morphine.
- Effective for mild to moderate pain.
- Constipation occurs
- Dizziness may occur in ambulatory patients.
- More potent histamine-releasing action than does morphine.
- Should not be administered by IV injection.
- Extremely effective antitussive agent and is used therapeutically for suppressing cough.
- In contrast to morphine, codeine overdose can occasionally lead to the production of seizures.
- Seizures can be treated with barbiturates.
- Respiratory depression can be counteracted with Naloxone.
- orally, 30 mg of codeine is equi-analgesic to 600 mg of aspirin, however, the effects of the two are additive, and occasionally synergistic
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.
Antiarrhythmic Drugs
Cardiac Arrhythmias
Can originate in any part of the conduction system or from atrial or ventricular muscle.
Result from
– Disturbances in electrical impulse formation (automaticity)
– Conduction (conductivity)
– Both
MECHANISMS OF ARRHYTHMIA
ARRHYTHMIA – absence of rhythm
DYSRRHYTHMIA – abnormal rhythm
ARRHYTHMIAS result from:
1. Disturbance in Impulse Formation
2. Disturbance in Impulse Conduction
- Block results from severely depressed conduction
- Re-entry or circus movement / daughter impulse
Types of Arrhythmias
• Sinus arrhythmias
– Usually significant only
– if they are severe or prolonged
• Atrial arrhythmias
– Most significant in the presence of underlying heart disease
– Serious: atrial fibrillation can lead to the formation of clots in the heart
• Nodal arrhythmias
– May involve tachycardia and increased workload of the heart or bradycardia from heart block
• Ventricular arrhythmias
– Include premature ventricular contractions (PVCs), ventricular tachycardia, and ventricular fibrillation
|
Class |
Action |
Drugs |
|
I |
Sodium Channel Blockade |
|
|
IA |
Prolong repolarization |
Quinidine, procainamide, disopyramide |
|
IB |
Shorten repolarization |
Lidocaine, mexiletine, tocainide, phenytoin |
|
IC |
Little effect on repolarization |
Encainide, flecainide, propafenone |
|
II |
Beta-Adrenergic Blockade |
Propanolol, esmolol, acebutolol, l-sotalol |
|
III |
Prolong Repolarization (Potassium Channel Blockade; Other) |
Ibutilide, dofetilide, sotalol (d,l), amiodarone, bretylium |
|
IV |
Calcium Channel Blockade |
Verapamil, diltiazem, bepridil |
|
Miscellaneous |
Miscellaneous Actions |
Adenosine, digitalis, magnesium |
Indications
• To convert atrial fibrillation (AF) or flutter to normal sinus rhythm (NSR)
• To maintain NSR after conversion from AF or flutter
• When the ventricular rate is so fast or irregular that cardiac output is impaired
– Decreased cardiac output leads to symptoms of decreased systemic, cerebral, and coronary circulation
• When dangerous arrhythmias occur and may be fatal if not quickly terminated
– For example: ventricular tachycardia may cause cardiac arrest
Mechanism of Action
• Reduce automaticity (spontaneous depolarization of myocardial cells, including ectopic pacemakers)
• Slow conduction of electrical impulses through the heart
• Prolong the refractory period of myocardial cells (so they are less likely to be prematurely activated by adjacent cells
Cells of the Nervous System
1-Neurons (Nerve Cells):function units of the nervous system by conducting nerve impulses, highly specialized and amitotic. Each has a cell body (soma), one or more dendrites, and a single axon.
• Cell Body: it has a nucleus with at least one nucleolus and many of the typical cytoplasmic organelles, but lacks centriolesfor cell division.
• Dendrites:Dendrites and axons are cytoplasmic extensions (or processes), that project from the cell body. They are sometimes referred to as fibers. Dendrites (afferent processes) increase their surface area to receive signals from other neurons, and transmit impulses to the neuron cell body.
• Axon: There is only one axon (efferent process) that projects from each cell body.
It carries impulses away from the cell body.
2-Glial cells: do not conduct nerve impulses, but support, nourish, and protect the neurons. They are mitotic, and far more numerous than neurons.
Astrocyte: A glialcell that provides support for neurons of the CNS, provides nutrients regulates the chemical composition of the extracellularfluid.
• Oligodendrocyte: A type of glialcell in the CNS that forms myelin sheaths.
• Microglia:The smallest glialcells; act as phagocytes (cleaning up debris) and protect the brain from invading microorganisms.
• Schwann cell:A cell in the PNS that is wrapped around a myelinatedaxon, providing one segment of its myelin sheath.