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Pharmacology - NEETMDS- courses
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Pharmacology

Osmotic diuretics

An osmotic diuretic is a type of diuretic that inhibits reabsorption of water and sodium. They are pharmacologically inert substances that are given intravenously. They increase the osmolarity of blood and renal filtrate.

Mechanism(s) of Action

1.    Reduce tissue fluid (edema) 
2.    Reflex cardiovascular effect by osmotic retention of fluid within vascular space which increases blood volume (contraindicated with Congestive heart failure) 
3.    Diuretic effect

o    Makes H2O reabsorption far more difficult for tubular segments insufficient Na & H2O capacity in distal segments
o    Increased intramedullary blood flow (washout)
o    Incomplete sodium recapture (asc. loop). this is indirect inhibition of Na reabsorption (Na stays in tubule because water stays) 
o    Net diuretic effect: 
    Tubular concentration of sodium decreases 
    Total amount of sodium lost amount increases 
    GFR unchanged or slightly increased

Toxicity

Circulatory overload, dilutional hyponatremia,  Hyperkalemia, edema, skin necrosis

Agents
Mannitol

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

Procaine penicillin Procaine penicillin is a combination of benzylpenicillin with the local anaesthetic agent procaine. This combination is aimed at reducing the pain and discomfort associated with a large intramuscular injection of penicillin.

Indications

respiratory tract infections where compliance with oral treatment is unlikely ,syphilis, cellulitis

Paracetamol

Paracetamol or acetaminophen is analgesic and antipyretic drug that is used for the relief of fever, headaches, and other minor aches and pains.

paracetamol acts by reducing production of prostaglandins, which are involved in the pain and fever processes, by inhibiting the cyclooxygenase (COX)  enzyme.

Metabolism Paracetamol is metabolized primarily in the liver. At usual doses, it is quickly detoxified by combining irreversibly with the sulfhydryl group of glutathione to produce a non-toxic conjugate that is eventually excreted by the kidneys.

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.

Drugs used to induce vomiting

In case of poisoning with noncorrosive agents, and assuming incomplete absorption of the poison has taken place, induction of vomiting can be carried out. One of the drugs used for this purpose is emetine which causes irritation of the upper gut and, on absorption, it also acts on  CTZ.  

Chemotherapeutic agents (or their metabolites) can directly activate the medullary chemoreceptor trigger zone or vomiting center; several neuroreceptors, including dopamine receptor Type 2 and serotonin Type 3 (5-HT3) from cell damage(GIT and pharynx) play roles in vomiting.

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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