NEET MDS Lessons
Pharmacology
Glucocorticoids
Cortisol (hydrocortisone) and its synthetic derivatives
Drug |
Duration |
Cortisol | Short |
Prednisone | Medium |
Triameinolone | Intermediate |
Betamethasone | Long |
Dexamethasone | Long |
Mechanism
↓ the production of leukotrienes and prostaglandins - inhibits phospholipase A2 , inhibits expression of COX-2 , will also stimulate the bone marrow to produce neutrophils resulting in leukocytosis
halts inflammatory cascade
↓ leukocyte migration
↓ capillary permeability
↓ phagocytosis
↓ platelet-activating factor
↓ interleukins (e.g. IL-2)
may trigger apoptosis in dividing and non-dividing cells
used in cancer chemotherapy
Clinical use
anti-inflammatory
immunosuppression
cancer chemotherapy (prednisone most common)
CLL
Hodgkin's lymphomas
part of MOPP regimen
Addison disease
asthma
Toxicity
1) must taper dose to avoid toxicity
2) suppression of ACTH → shock state if abrupt withdrawal - > cortical atrophy, malaise, myalgia, arthralgia, fever
3) iatrogenic Cushing syndrome ->buffalo hump, moon facies, truncal obesity, muscle weakness and atrophy, thin skin, easy bruising, acne
4) osteoporosis - vertebral fractures, aseptic hip necrosis, ↓ skeletal growth in children
5) hyperglycemia (diabetes) -due to ↑ gluconeogenesis , glaucoma, cataracts, and other complications can subsequently result
6) ↑ GI acid release -ulcers
7) Na+ retention -> edema, HTN, hypokalemia alkalosis, hypocalcemia
8)↓ wound healing
9) ↑ infections
10) mental status changes
11) cataracts
Needle selection
Nerve blocks:
Inferior alveolar- 25 G short (LLU technique)
PSA- 25 G short
Mental/Incisive- 25 G short
Palatal- 27/30 G short/ultrashort
Gow-Gates/Akinosi- 25 G long
Infraorbital- 25 G long
Field Block:
ASA 25/27 short
Infiltration:
Infiltration/SP 25/27 short
PDL/Intraosseous
PDL 27/30 short
Intraosseous 30 short/ultrashort
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
Benzodiazepines
All metabolites are active sedatives except the final glucuronide product.
Elimination half-life varies a great deal from drug to drug.
?-Hydroxylation is a rapid route of metabolism that is unique to triazolam,
midazolam, and alprazolam.
This accounts for the very rapid metabolism and short sedative actions of these
drugs.
Pharmacological effects of benzodiazepines
- Antianxiety.
- Sedation.
- Anticonvulsant (including drug-induced convulsions).
- Amnesia, especially drugs like triazolam.
- Relax skeletal muscle (act on CNS polysynaptic pathways).
Indications
- IV sedation, (e.g., midazolam, diazepam, lorazepam).
- Antianxiety.
- Sleep induction.
- Anticonvulsant (e.g., diazepam, clonazepam).
- Panic disorders.
- Muscle relaxation.
Adverse effects
- Ataxia, confusion.
- Excessive sedation.
- Amnesia (not a desired effect with daytime sedation).
- Altered sleep patterns (increase stage 2 and decrease stage 4 sleep).
Barbiturates
1. Long-acting. Phenobarbital is used to treat certain types of seizures (see section on antiepileptic drugs).
2. Intermediate-acting. Amobarbital, pentobarbital (occasionally used for sleep), secobarbital.
3. Short-acting. Hexobarbital, methohexital, thiopental—rarely used as IV anesthetics.
Enflurane (Ethrane) MAC 1.68, Blood/gas solubility ratio 1.9
- Extremely stable chemically.
- Less potent and less soluble in blood than is halothane.
- Respiratory depression is similar to that seen with halothane.
- Cardiac output is not depressed as much as with halothane, and the heart is not sensitized to catecholamines to the same degree.
- Enflurane produces better muscle relaxation than does halothane.
- Metabolism of this agent is very low. Inorganic fluoride is a product of metabolism, but is not sufficient to cause renal problems.
- Enflurane differs from halothane and the other inhalational anesthetic agents by causing seizures at doses slightly higher than those that induce anesthesia.
- Nausea appears to occur somewhat more often following Enflurane than it does following halothane.
Aminoglycoside
Aminoglycosides are a group of antibiotics that are effective against certain types of bacteria. They include amikacin, gentamicin, kanamycin, neomycin, netilmicin, paromomycin, streptomycin, and tobramycin. Those which are derived from Streptomyces species
Aminoglycosides work by binding to the bacterial 30S ribosomal subunit, causing misreading of t-RNA, leaving the bacterium unable to synthesize proteins vital to its growth.
Aminoglycosides are useful primarily in infections involving aerobic, Gram-negative bacteria, such as Pseudomonas, Acinetobacter, and Enterobacter. In addition, some mycobacteria, including the bacteria that cause tuberculosis, are susceptible to aminoglycosides. Streptomycin was the first effective drug in the treatment of tuberculosis, though the role of aminoglycosides such as streptomycin and amikacin have been eclipsed (because of their toxicity and inconvenient route of administration) except for multiple drug resistant strains.
Infections caused by Gram-positive bacteria can also be treated with aminoglycosides, but other types of antibiotics are more potent and less damaging to the host. In the past the aminoglycosides have been used in conjunction with penicillin-related antibiotics in streptococcal infections for their synergistic effects, particularly in endocarditis.
Because of their potential for ototoxicity and renal toxicity, aminoglycosides are administered in doses based on body weight. Blood drug levels and creatinine are monitored during the course of therapy.
There is no oral form of these antibiotics: they are generally administered intravenously, though some are used in topical preparations used on wounds.
Aminoglycosides are mostly ineffective against anaerobic bacteria, fungi and viruses.