NEET MDS Lessons
Pharmacology
Sympathomimetics
Beta-Adrenergic Agonists
Beta1-adrenergic agonists (dopamine, dobutamine, prenalterol, xamoterol) have been used to treat acute and chronic heart failure, but have limited usefulness in chronic CHF because of their arrhythmogenic effects, short duration of action, the development of tolerance, and necessity of parenteral administration
Dopamine (i.v.) is used in acute heart failure (cardiogenic shock) to increase blood pressure and increase cardiac output
- It has a short half-life (1 min)
- At high doses dopamine has potent peripheral vasoconstrictor effects (alpha-receptor stimulation), in addition to its inotropic effects
- Low dose dopamine has a renal artery dilating effect and may improve sodium and water excretion in patients refractory to loop diuretics
- When systolic pressure is greater than 90 mm Hg, nitroprusside can be added to reduce ventricular filling pressure and reduce afterload
- i.v. furosemide should also be administered to reduce edema
Levodopa and ibopamine, analogs of dopamine that can be administered orally, have been shown to improve symptoms in some patients, but can exhibit arrhythmogenic side-effects and tachyphylaxis
Dobutamine is a somewhat selective beta1-adrenergic agonist that lacks vasoconstrictor activity and causes minimal changes in heart rate
- It is frequently added to nitroprusside when blood pressure is adequate to increase cardiac output
- It is administered as an i.v. infusion to treat acute severe heart failure
- It has a short half-life (2.4 min) and is only used on a short-term basis, although long-term beneficial effects on cardiac function have been noted
- After 72 hours of therapy, tolerance can develop to dobutamine necessitating switch to other inotropic support (e.g. milrinone)
- Dobutamine can enhance AV conduction and worsen atrial tachycardia
Prenalterol and xamoterol are partial beta1-adrenergic agonists that may simultaneously stimulate beta1-receptors and block the receptors from stimulation by endogenous catecholamines, thereby protecting against beta1-receptor down-regulation
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 .
Cough is a protective reflex which helps in expulsion of respiratory secretion or foreign particles which are irritant to respiratory
tract. Irritation to any part of respiratory tract starting from pharynx to lungs carried impulses by afferent fibres in vagus and
sympathetic nerve to the cough centre in the medulla oblongata. \
Cough may be dry (without sputum or unproductive) or productive (with sputum production).
Classification for drugs used in cough.
I. Pharyngeal demulcents
Certain lozenges, linctus and cough drops containing glycerine, liquorice and syrups.
II. Expectorants
Sodium and potassium citrate
Sodium and potassium acetate
Potassium iodide
Ammonium chloride & carbonate
Acetylcysteine
Bromhexine
Guaiphenesin
III. Antitussive
i. Opioids
Codeine (as linctus) Pholcodeine
ii. Non-opioids
Noscapine
Dextromethorphan
Pipazethate
iii. Antihistaminics
Chlorpheniramine
Diphenhydramine
Promethazine
Erdosteine is recently introduced mucolytic with unique protective functions for the respiratory tract. It is indicated in the treatment of acute and chronic airway diseases such as bronchitis, rhinitis, sinusitis, laryngopharyngitis and exacerbations of chronic bronchitis.
Agonist, Antagonist, and Partial Agonists
Agonists: molecules that activate receptors. A drug that mimics the body's own regulatory processes.
Antagonists: produce their effects by preventing receptors activation by endogenous regulatory molecules and drugs. Block activation of receptors by agonists.
Noncompetive Antagonist: Bind irreversibly to receptors, and reduce the maximal response that an agonist can elicit.
Competitive Antagonist: Bind reversibly to receptors, competing with agonists for binding sites.
Partial Agonists: Have moderate intrinsic activity, the maximal effect that a partial agonist can produce is lower than that of a full agonist. Act as antagonists as well as agonists.
Nalidixic acid:
Nalidixic acid is the basis for quinolone antibiotics. It acts bacteriostatically (that is, it inhibits growth and reproduction) or bactericidally (it kills them) on both Gram positive and Gram negative bacteria, depending on the concentration. It is especially used in treating urinary tract infections, caused for example by Escherichia coli, Proteus, Enterobacter and Klebsiella.
Operator position
For the right-handed operator, the 8 and 10 o’clock position and for left-handed operators, the corresponding 2 and 4 o’clock position almost always allows for optimal visualization of the injection field.
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