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Pharmacology

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

PSEUDOEPHEDRINE

Pseudoephedrine appears to have less pressor activity and weaker central nervous system effects than ephedrine. It has agonist activity at both β1  and β2 adrenoceptors, leading to increased cardiac output and relaxation of bronchial smooth muscle.

Pseudoephedrine is rapidly absorbed throughout the body. It is eliminated largely unchanged in urine by N-demethylation.

It is indicated in symptomatic relief from stuffed nose, respiratory tract congestion, bronchospasm associated with asthma, bronchitis and other similar disorders.

DIURETICS

Specific Therapeutic Objective

Clinical State(s)

Drug(s) (Class)

Draw fluid from tissue to vascular space reduce tissue edema

Cerebral edema
glaucoma

Mannitol (Osmotic)
Glucose (Osmotic)
Glycerin (Osmotic)

Decrease renal swelling
expand tubular volume

Renal shutdown

Glucose (Osmotic)
Mannitol (Osmotic)

Modest and/or sustained decrease in venous hydrostatic pressure

Congestive heart failure
Hepatic cirrhosis
Udder edema

Hydrochlorothiazide (thiazide)
Chlorothiazide (thiazide)

Aggressive and/or short-term decrease in venous hydrostatic pressure

Congestive heart failure
Hepatic cirrhosis
Udder edema

Furosemide (loop)

Inhibit aldosterone action

Hepatic cirrhosis
Congestive heart failure

triamterene (K+ sparing)
spironolactone (K+ sparing - competitive)

Reduce potassium wasting 2o to other diuretic

Hepatic cirrhosis
Congestive heart failure

triamterene (K+ sparing)
spironolactone (K+ sparing - competitive)

Inhibit ADH action

Inappropriate ADH secretion

lithium (aquaretic)
demeclocycline (aquaretic

Increase calcium secretion

Malignant hypercalcemia

  • Paraneoplastic
  • Hypervitaminosis D

Furosemide (loop)

Reduce urine output

Diabetes insidpidus

Hydrochlorothiazide (thiazide)
Chlorothiazide (thiazide)

Urine alkalinization

Various

Carbonic anhydrase inhibitors

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

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

Effects and Toxic Actions on Organ Systems

1. Local anesthetics (dose dependent) interfere with transmission in any excitable tissue (e.g. CNS and CVS).

2. CNS effects

 a. Central neurons very sensitive.

 b. Excitatory-dizziness, visual and auditory disturbances, apprehension, disorientation and muscle twitching more common with ester type agents.

 c. Depression manifested as slurred speech, drowsiness and unconsciousness more common with amide type agents (e.g. lidocaine).

 d. Higher concentrations of local anesthetic may eventually produce tonic-clonic[grand mal]  convulsions.

 e. Very large doses may produce respiratory depression which can be fatal. Artificial respiration may be life-saving.

 3.CVS effects

 a. Local anesthetics have direct action on the myocardium and peripheral vasculature by closing the sodium channel, thereby limiting the inward flux of sodium ions.

 b. Myocardium usually depressed both in rate and force of contraction. Depression of ectopic pacemakers useful in treating cardiac arrhythmias.

 c. Concentrations employed clinically usually cause vasodilation in area of injection.

 d. Vasoconstrictors such as epinephrine may counteract these effects on myocardium and vasculature.

4.  Local Tissue Responses

 a. Occasionally focal necrosis in skeletal muscle at injection site, decreased cell motility and delayed wound healing.

 b. Tissue hypoxia may be produced by action of excessive amounts of vasoconstrictors.

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 

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