NEET MDS Lessons
Pharmacology
Antidiarrheal
Antidiarrheal drugs may be given to relieve the symptom (non-specific therapy) or may be given to treat the underlying cause of the symptom (specific therapy).
Ι. Drugs used for the symptomatic (non-specific) treatment of diarrhoea include:
• Opiates and opiate derivatives are the most effective (such as morphine), but it is not used because of potentially serious adverse effects. Other agents, such as diphenoxylate and loperamide, are commonly used.
• Adsorbent – demulcent products such as kaolin – pectin preparation may be included in antidiarrheal preparations. Unfortunately, they may adsorb nutrients and other drugs, including the antidiarrheal agents if given concurrently.
• Anticholinergic agents e.g. atropine is occasionally used to decrease abdominal cramping and pain associated with diarrhoea.
ΙΙ. Specific therapy may include the use of antibacterial agents that are recommended for use in carefully selected cases of bacterial enteritis. For example, severe diarrhoea by salmonella, shigella, campylobacter and clostridia species can be treated by antibiotics (ampicillin, chloramphenicol, co-trimoxazole).
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
Anesthesia agents
1. Inhalation anesthetics (volatile anesthetics)
- gases : N2O, xenon
- Fluids (vaporisers)
2. Intravenous anesthetics
- Barbiturans : thiopental
- Others : propofol, etomidat
3. Pain killers
- Opioids: fentanyl, sufentanil, alfentanil, remifentanil, morphine
- Non Steroid Anti Inflamatory Drugs: ketonal, paracetamol
4. Relaxants
- Depolarising : succinilcholine
- Non depolarising : atracurium, cisatracurium, vecuronium, rocuronium
5. adiuvants
-benzodiazepins: midasolam, diazepam
Pharmacodynamic Effects of NSAIDs
A. Positive
analgesic - refers to the relief of pain by a mechanism other than the reduction of inflammation (for example, headache);
- produce a mild degree of analgesia which is much less than the analgesia produced by opioid analgesics such as morphine
anti-inflammatory - these drugs are used to treat inflammatory diseases and injuries, and with larger doses - rheumatoid disorders
antipyretic - reduce fever; lower elevated body temperature by their action on the hypothalamus; normal body temperature is not reduced
Anti-platelet - inhibit platelet aggregation, prolong bleeding time; have anticoagulant effects
B. Negative
Gastric irritant
Decreased renal perfusion
Bleeding
(CNS effects)
Adverse effects
The two main adverse drug reactions (ADRs) associated with NSAIDs relate to gastrointestinal (GI) effects and renal effects of the agents.
Gastrointestinal ADRs
The main ADRs associated with use of NSAIDs relate to direct and indirect irritation of the gastrointestinal tract (GIT). NSAIDs cause a dual insult on the GIT - the acidic molecules directly irritate the gastric mucosa; and inhibition of COX-1 reduces the levels of protective prostaglandins.
Common gastrointestinal ADRs include:
Nausea, dyspepsia, ulceration/bleeding, diarrhoea
Risk of ulceration increases with duration of therapy, and with higher doses. In attempting to minimise GI ADRs, it is prudent to use the lowest effective dose for the shortest period of time..
Ketoprofen and piroxicam appear to have the highest prevalence of gastric ADRs, while ibuprofen (lower doses) and diclofenac appear to have lower rates.
Commonly, gastrointestinal adverse effects can be reduced through suppressing acid production, by concomitant use of a proton pump inhibitor, e.g. omeprazole
Renal ADRs
NSAIDs are also associated with a relatively high incidence of renal ADRs. The mechanism of these renal ADRs is probably due to changes in renal haemodynamics (bloodflow), ordinarily mediated by prostaglandins, which are affected by NSAIDs.
Common ADRs associated with altered renal function include:
salt and fluid retention,hypertension
These agents may also cause renal impairment, especially in combination with other nephrotoxic agents. Renal failure is especially a risk if the patient is also concomitantly taking an ACE inhibitor and a diuretic - the so-called "triple whammy" effect.
In rarer instances NSAIDs may also cause more severe renal conditions.
interstitial nephritis, nephrotic syndrome, acute renal failure
Photosensitivity
Photosensitivity is a commonly overlooked adverse effect of many of the NSAIDs. These antiinflammatory agents may themselves produce inflammation in combination with exposure to sunlight. The 2-arylpropionic acids have proven to be the most likely to produce photosensitivity reactions, but other NSAIDs have also been implicated including piroxicam, diclofenac and benzydamine.
ibuprofen having weak absorption, it has been reported to be a weak photosensitising agent.
Other ADRs
Common ADRs, other than listed above, include: raised liver enzymes, headache, dizziness.
Uncommon ADRs include: heart failure, hyperkalaemia, confusion, bronchospasm, rash.
The COX-2 paradigm
It was thought that selective inhibition of COX-2 would result in anti-inflammatory action without disrupting gastroprotective prostaglandins.
The relatively selective COX-2 oxicam, meloxicam, was the first step towards developing a true COX-2 selective inhibitor. Coxibs, the newest class of NSAIDs, can be considered as true COX-2 selective inhibitors and include celecoxib, rofecoxib, valdecoxib, parecoxib and etoricoxib.
Valdecoxib
used in the treatment of osteoarthritis, acute pain conditions, and dysmenorrhoea
Etoricoxib new COX-2 selective inhibitor
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
Propofol -Intravenous Anesthetics
- A nonbarbiturate anesthetic
- It is very lipid-soluble, acts rapidly and has a short recovery time.
- It is associated with less nausea and vomiting than some of the other IV anesthetics.
- Propofol is very similar to thiopental in its effects on the cardiorespiratory system.
- It does not have any analgesic properties but lowers the dose of opioid needed when the two agents are used in combination.
- The most significant adverse cardiovascular effect associated with propofol administration is hypotension. It should be used with caution in patients with cardiac disease.