NEET MDS Lessons
Pharmacology
Carbapenems: Broadest spectrum of beta-lactam antibiotics.
imipenem with cilastatin
meropenem
ertapenem
Monobactams: Unlike other beta-lactams, there is no fused ring attached to beta-lactam nucleus. Thus, there is less probability of cross-sensitivity reactions.
aztreonam
Beta-lactamase Inhibitors No antimicrobial activity. Their sole purpose is to prevent the inactivation of beta-lactam antibiotics by beta-lactamases, and as such, they are co-administered with beta-lactam antibiotics.
clavulanic acid
tazobactam
sulbactam
Example calculations of maximum local anesthetic doses for a 15-kg child
Articaine
5 mg/kg maximum dose × 15 kg = 75 mg
4% articaine = 40 mg/mL
75 mg/(40 mg/mL) = 1.88 mL
1 cartridge = 1.8 mL
Therefore, 1 cartridge is the maximum
Lidocaine
7 mg/kg × 15 kg = 105 mg
2% lidocaine = 20 mg/mL
105 mg/(20 mg/mL) = 5.25 mL
1 cartridge = 1.8 mL
Therefore, 2.9 cartridges is the maximum
Mepivacaine
6.6 mg/kg × 15 kg = 99 mg
3% mepivacaine = 30 mg/mL
99 mg/(30 mg/mL) = 3.3 mL
1 cartridge = 1.8 mL
Therefore, 1.8 cartridges is the maximum.
Prilocaine
8 mg/kg × 15 kg = 120 mg
4% prilocaine = 40 mg/mL
120 mg/(40 mg/mL) = 3 mL
1 cartridge = 1.8 mL
Therefore, 1.67 cartridges is the maximum
Mefenamic acid
Analgesic, anti‐inflammatory properties less effective than aspirin
Short half‐lives, should not be used for longer than one week and never in pregnancy and in children.
Enhances oral anticoagulants
Used to treat pain, including menstrual pain. It decreases inflammation (swelling) and uterine contractions.
OXYMETAZOLINE
It is a directly acting sympathomimetic amine used in symptomatic relief in nasal congestion which increases mucosal secretion.
It is used:
- As a nasal decongestant in allergic rhinitis, with or without the addition of antazoline or sodium chromoglycate.
- As an ocular decongestant in allergic conjunctivitis.
Compounds like naphazoline and xylometazoline are relatively selective α2 agonists, which on topical application produce local vasoconstriction.
ANTIDEPRESSANTS
Monoamine uptake inhibitors
1. Tricyclic antidepressants (TCAs)
2. Selective serotonin reuptake inhibitors (SSRIs)
3. Serotonin-norepinephrine reuptake inhibitors(SNRIs)
4. Norepinephrine reuptake inhibitor
Monoamine oxidase inhibitors (MAOIs)
Monoamine receptor antagonists
Fentanyl (Sublimaze)
- Related chemically to meperidine.
- Approximately 80 times more potent than morphine.
- Duration of action very short (t1/2 20 min).
- Used mainly following general anesthesia.
- Neurolept analgesia: Fentanyl & Droperidol (Innovar)
- fentanyl in analgesic (2-10 µg/kg), or anaesthetic (30-100 µg/kg) doses seldom causes significant decreases in blood pressure when given alone, even in patients with poor LV function
- hypotension following fentanyl is mostly due to bradycardia and can be prevented by the use of anticholinergics, sympathomimetics or agents such as pancuronium this is more likely to occur in patients with high pre-existing sympathetic tone
- hypertension is the commonest disturbance with high dose fentanyl anaesthesia, usually accompanying intubation, sternotomy, or aortic root dissection
Class I Sodium Channel Blockers
• Block movement of sodium into cells of the cardiac conducting system
• Results in a stabilizing effect and decreased formation and conduction of electrical impulses
• Have a local anesthetic effect
• Are declining in use due to proarrhythmic effects and increased mortality rates
• Na channel blockers - Class 1 drugs are divided into 3 subgroups
• 1A. 1B, 1C based on subtle differences in their mechanism of action.
• Blockade of these channels will prevent depolarization.
• Spread of action potential across myocardium will slow and areas of pacemaker activity is suppressed.
Class IA Sodium Channel Blockers
• Treatment of: symptomatic premature ventricular contractions, supraventricular tachycardia, and ventricular tachycardia, prevention of ventricular fibrillation
– Quinidine (Cardioquin, Quinaglute)
– Procainamide (Pronestyl, Procanbid)
– Disopyramide (Norpace)
• Quinidine – prototype
• Low therapeutic index
• High incidence of adverse effects
Class IB Sodium Channel Blockers
• Treatment of: symptomatic premature ventricular contractions and ventricular tachycardia, prevention of ventricular fibrillation
– Lidocaine (Xylocaine)
– Mexiletine (Mexitil)
– Tocainide (Tonocard)
– Phenytoin (Dilantin)
Side Effects: Lidocaine
• Drowsiness • Paresthesias • Muscle twitching • Convulsions • Changes in mental status (disorientation, confusion) • Hypersensitivity reactions (edema, uticaria, anaphylaxis)
Side Effects: Phenytoin (Dilantin)
• Gingival hyperplasia
• Nystagmus
• Ataxia, slurring of speech
• Tremors
• Drowsiness
• Confusion
• Lidocaine – prototype
• Must be given by injection
• Used as a local anesthetic
• Drug of choice for treating serious ventricular arrhythmias associated with acute myocardial infarction, cardiac surgery, cardiac catheterization and electrical conversion
Class IC Sodium Channel Blockers
• Treatment of: life-threatening ventricular tachycardia or fibrillation and supraventricular tachycardia unresponsive to other drugs
– Flecainide
– Propafenone
Adverse Effects
• CNS - dizziness, drowsiness, fatigue, twitching, mouth numbness, slurred speech vision changes, and tremors that can progress to convulsions.
• GI - changes in taste, nausea, and vomiting. CV - arrhythmias including heart blocks, hypotension, vasodilation, and potential for cardiac arrest.
• Other Rash, hypersensitivity reactions loss of hair and potential bone marrow depression.
Drug-Drug Interactions
• Increased risk for arrhythmias if combined with other drugs that are know to cause arrhythmias- digoxin and beta blockers
• Increased risk of bleeding if combined with oral anticoagulants.
Drug Food Interactions
• Quinidine needs an acidic urine for excretion. Increased levels lead to toxicity
• Avoid foods that alkalinize the urine- citrus juices, vegetables, antacid, milk products