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Pharmacology

Thiopental 

- A barbiturate that is generally used to induce anesthesia.
- The temporal course of effects from induction to recovery depends almost entirely upon progressive redistribution.
- Metabolic degradation or excretion during anesthesia is negligible, except in the case of methohexital.
- The barbiturates produce minimal analgesia.
- Respiratory depression may be pronounced.
- Cardiac output is reduced while total peripheral resistance is increased.
- It does not sensitize the heart to catecholamines.
- It may cause bronchiospasm, especially in asthmatics.
- It is contraindicated in acute intermittent porphyria.

ANTIASTHMATIC AGENTS

 Classification for antiasthmatic drugs.
 
I. Bronchodilators

i. Sympathomimetics (adrenergic receptor agonists)

Adrenaline, ephedrine, isoprenaline, orciprenaline, salbutamol, terbutaline, salmeterol, bambuterol

ii. Methylxanthines (theophylline and its derivatives)

Theophylline 
Hydroxyethyl theophylline 
Theophylline ethanolate of piperazine

iii. Anticholinergics

Atropine methonitrate 
Ipratropium bromide

II. Mast cell stabilizer

Sodium cromoglycate
Ketotifen 


III. Corticosteroids

Beclomethasone dipropionate 
Beclomethasone (200 µg) with salbutamol

IV. Leukotriene pathway inhibitors 

Montelukast 
Zafirlukast

Pramlintide -Amylin mimetics

Mechanism
synthetic analogue of human amylin that acts in conjunction with insulin
↓ release of glucagon
delays gastric emptying

Clinical use

type I and II DM

Treatment modifications to consider if there are concerns regarding vasoconstrictors

- Monitor blood pressure and heart rate preoperatively

- Minimize administration of epinephrine or levonordefrin

- Monitor blood pressure and heart rate 5 min after injection

- May re-administer epinephrine or levonordefrin if blood pressure and heart rate are stable

- Continue to monitor as required

- Consider limiting epinephrine to 0.04 mg, levonordefrin to 0.2 mg

- Avoid epinephrine 1:50,000

- Never use epinephrine-impregnated retraction cord

COAGULANTS

An agent that produces coagulation (Coagulation is a complex process by which blood forms clots).

ANTICOAGULANTS

An anticoagulant is a substance that prevents coagulation; that is, it stops blood from clotting.

 

Anticoagulants:

Calcium Chelators (sodium citrate, EDTA)

Heparin

Dalteparin Sodium (Fragmin) -Low molecular-weight heparin

Enoxaparin - Low molecular-weight heparin

Tinzaparin Sodium  - Low molecular-weight heparin

Warfarin

Lepirudin - recombinant form of the natural anticoagulant hirudin: potent and specific Thrombin inhibitor

Bivalirudin - analog of hirudin: potent and specific Thrombin inhibitor

Procoagulants:

Desmopressin acetate

Antiplatelet Drugs:

Acetylsalicylic Acid, Ticlopidine, Sulfinpyrazone, Abciximab , Clopidogrel bisulfate

Fibrinolytic Drugs:

Tissue Plasminogen Activator (t-PA, Activase), Streptokinase (Streptase),

Anistreplase, Urokinase

 

Antagonists:

Protamine sulfate, Aminocaproic acid

Pharmacological agents used to treat blood coagulation disorders fall in to three major categories:

1. Anticoagulants: Substances that prevent the synthesis of a fibrin network which inhibits coagulation and the formation of arterial thrombi and thromboembolic clots.

2. Antiplatelet agents: Substances that reduce the adhesion and aggregation of platelets.

3. Fibrinolytic agents: Substances that promote the destruction of already formed blood clots or thrombi by disrupting the fibrin mesh.

Ethosuximide (Zarontin): use in absence seizures (may exacerbate tonic-clonic seizures)

Mechanism: ↓ T-type Ca currents in thalamic neurons, inhibits bursts of APs, ↓ synchronous neuronal firing
i.    Thalamo-cortical reverberating circuits: during absence type seizures, have reverberating circuits between cerebral cortex and thalamus at 3 Hz maintained by T-type Ca channels (since blocking these channels blocks the reverberating circuit)


Side effects: quite non-toxic; common= N/V and anorexia; less common = headache, sedation, photophobia

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). 

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