NEET MDS Lessons
Pharmacology
Procoagulant Drugs:
Desmospressin Acetate
• Is a synthetic analogue of the pituitary antidiuretic hormone (ADH).
• Stimulates the activity of Coagulation Factor VIII
• Use for treatment of hemophilia A with factor VIII levels less than or equal to 5%, treatment of hemophilia B or in clients who have factor VIII antibodies. Treatment of severe classic von Willebrand's disease (type I) and when an abnormal molecular form of factor VIII antigen is present. Use for type IIB von Willebrand's disease.
AUTOCOIDS
An organic substance, such as a hormone, produced in one part of organism and transported by the blood or lymph to another part of the organism where it exerts a physiologic effect on that part.
TYPES OF AUTACOIDS:
Amines : Histamine,5-Hydroxytryptamine.
Lipids : Prostaglandins, Leukotriens, Platelet activating factor.
Peptide : Bradykinin , angiotensin.
SYMPATHOMIMETICS
β2 -agonists are invariably used in the symptomatic treatment of asthma.
Epinephrine and ephedrine are structurally related to the catecholamine norepinephrine, a neurotransmitter of the adrenergic nervous system
Some of the important β 2 agonists like salmeterol, terbutaline and salbutamol are invariably used as bronchodilators both oral as well as
aerosol inhalants
SALBUTAMOL
It is highly selective β2 -adrenergic stimulant h-aving a prominent bronchodilator action.
It has poor cardiac action compared to isoprenaline.
TERBUTALINE
It is highly selective β2 agonist similar to salbutamol, useful by oral as well as inhalational route.
SALMETEROL
Salmeterol is long-acting analogue of salbutamol
BAMBUTEROL
It is a latest selective adrenergic β2 agonist with long plasma half life and given once daily in a dose of 10-20 mg orally.
METHYLXANTHINES (THEOPHYLLINE AND ITS DERIVATIVES)
THEOPHYLLINE
Theophylline has two distinct action:
smooth muscle relaxation (i.e. bronchodilatation) and suppression of the response of the airways to stimuli (i.e. non-bronchodilator prophylactic effects).
ANTICHOLINERGICS
Anticholinergics, like atropine and its derivative ipratropium bromide block cholinergic pathways that cause airway constriction.
MAST CELL STABILIZERS
SODIUM CROMOGLYCATE
It inhibits degranulation of mast cells by trigger stimuli.
It also inhibits the release of various asthma provoking mediators e.g. histamine, leukotrienes, platelet activating factor (PAF) and interleukins (IL’s) from mast cell
KETOTIFEN
It is a cromolyn analogue. It is an antihistaminic (H1 antagonist) and probably inhibits airway inflammation induced by platelet activating factor (PAF) in primate.
It is not a bronchodilator. It is used in asthma and symptomatic relief in atopic dermatitis, rhinitis, conjunctivitis and urticaria.
LEUKOTRIENE PATHWAY INHIBITORS
MONTELUKAST
It is a cysteinyl leukotriene receptor antagonist indicated for the management of persistent asthma.
Meperidine (Demerol)
Meperidine is a phenylpiperidine and has a number of congeners. It is mostly effective in the CNS and bowel
- Produces analgesia, sedation, euphoria and respiratory depression.
- Less potent than morphine, 80-100 mg meperidine equals 10 mg morphine.
- Shorter duration of action than morphine (2-4 hrs).
- Meperidine has greater excitatory activity than does morphine and toxicity may lead to convulsions.
- Meperidine appears to have some atropine-like activity.
- Does not constrict the pupils to the same extent as morphine.
- Does not cause as much constipation as morphine.
- Spasmogenic effect on GI and biliary tract smooth muscle is less pronounced than that produced by morphine.
- Not an effective antitussive agent.
- In contrast to morphine, meperidine increases the force of oxytocin-induced contractions of the uterus.
- Often the drug of choice during delivery due to its lack of inhibitory effect on uterine contractions and its relatively short duration of action.
- It has serotonergic activity when combined with monoamine oxidase inhibitors, which can produce serotonin toxicity (clonus, hyperreflexia, hyperthermia, and agitation)
Adverse reactions to Meperidine
• Generally resemble a combination of opiate and atropine-like effects.
- respiratory depression, - tremors, - delirium and possible convulsions, - dry mouth
• The presentation of mixed symptoms (stupor and convulsions) is quite common in addicts taking large doses of meperidine.
SGLT-2 Inhibitors
canagliflozin
empagliflozin
Mechanism
glucose is reabsorbed in the proximal tubule of the nephron by the sodium-glucose cotransporter 2 (SGLT2)
SGLT2-inhibitors lower serum glucose by increasing urinary glucose excretion
the mechanism of action is independent of insulin secretion or action
Clinical use
type II DM
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.
Ether (diethylether)
Ether (diethylether) MAC 2.0%, Blood/gas solubility ratio 15
- Ether is generally mixed with 3% ethanol to retard oxidation. Peroxides form on exposure to air and can enhance the danger of an explosion.
- Slow rate of induction and recovery due to its high blood/gas solubility ratio.
- Produces profound muscular relaxation.
- Both the rate and the minute volume of ventilation tend to be elevated during the inhalation of ether.
- Ether maintains good circulatory stability and does not sensitize the heart to the arrhythmogenic action of catecholamines.
- More than 90% of the absorbed ether can be recovered unchanged in the expired air. Metabolism is not extensive and the metabolites are not hepatotoxic.
- Ether is a versatile anesthetic of unexcelled safety, but it is flammable and irritating to breathe. Secretions can be blocked with anticholinergics.