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Pharmacology

Aquaretics
An aquaretic is a class of drug that is used to promote aquaresis, the excretion of water without electrolyte loss.

Lithium, demeclocycline

Mechanism of Action

1.    Block ADH action on distal tubule and collecting duct. Blocking ADH decreases H2O permeability. H2O is not recovered (distal tubule) using osmotic draw of counter-current multiplier so aquaretics reduce water reabsorption (tubule to blood stream). 
2.    Net effect is an increase in free water clearance
 

CLASSICATION OF ANTICOAGULANT DRUGS

1. Direct Acting Anticoagulants

a) Calcium Chelators (sodium citrate, EDTA)

b) Heparin

2. Indirect Acting Anticoagulant Drugs

a) Warfarin

Class III Potassium Channel Blockers

Prolong effective refractory period by prolonging Action Potential

Treatment: ventricular tachycardia and fibrillation, conversion of atrial fibrillation or flutter to  sinus rhythm, maintenance of sinus rhythm
– Amiodarone (Cordarone) – maintenance of sinus rhythm
– Bretylium (Bretylol) 
– Ibutilide (Corvert) 
– Dofetilide (Tykosyn) 
– Sotalol (Betapace) 

 

 Amiodarone 
- Has characteristics of sodium channel blockers, beta blockers, and calcium channel blockers 
- Has vasodilating effects and decreases systemic vascular resistance 
- Prolongs conduction in all cardiac tissue 
- Decreases heart rate 
- Decreases contractility of the left ventricles 

Class III - Adverse Effects 
- GI- Nausea vomiting and GI distress 
- CNS- Weakness and dizziness
- CV-Hypotension, CHF, and arrhythmias are common. 
- Amiodarone associated with potentially fatal Hepatic toxicity, ocular abnormalities and serious cardiac arrhythmias. 

Drug – Drug Interactions
These drugs can cause serious toxic effects if combined with digoxin or quinidine. 
 

Factors affecting onset and duration of action of local anesthetics

pH of tissue

pKa of drug

Time of diffusion from needle tip to nerve

Time of diffusion away from nerve

Nerve morphology

Concentration of drug

Lipid solubility of drug

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.

Chloral hydrate

1. Short-acting sleep inducer—less risk of “hangover” effect the next day.
2. Little change on REM sleep.
3. Metabolized to trichloroethanol, an active metabolite; further metabolism inactivates the drug.
4. Used for conscious sedation in dentistry.
5. Can result in serious toxicity if the dose is not controlled.

GENERAL ANESTHETICS

General anesthesia often involves more than one drug to get different, favourable effects.
Premedication is often used to:
1. Treat anxiety - Benzodiazapenes
2. Reduce pain - Opiod anaglesics such as morphine
3. Produce muscle paralysis -E.g. Tubocurare
4. Reduce secretions
Induction of anesthesia is often done via intravenous anesthetics, which are quick and easy to administer.
Maintenance of anesthesia involves inhalation agents.

Prototype Agents:
Volatile Anesthetics:
•    Nitrous Oxide
•    Ether
•    Halothane
•    Enflurane
•    Isoflurane

Injectable Anesthetics:
•    Thiopental 
•    Ketamine
•    Etomidate
•    Propofol 
•    Midazolam
 

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