Pharma written Flashcards
Give an account about asthma therapy ?
Bronchodilator drugs: like beta agonist, antimuscarinic drugs, methylxathines
Anti-inflammatory drugs like corticoids, leukotriene antagonist and mast cell stabilizers
Mechanism of action of beta agonist
B2 receptor stimulation–> activates adenyl cyclase —-> increase cAMP—->bronchodilatation
inhibit bronchoconstrictor mediators from mast cells
Increase ciliary activity
Salmeterol & Formoterol should not be used as monotherapy
Because they have no anti-inflammatory action they should not be used as monotherapy for asthma. Should be combined with corticosteroids as long term control medications of asthma
What are the adverse effects of Beta agonist?
Tachycardia
Tremors
Nervous tension
Tolerance
Hypokalemia due to increase activity of the Na/K ATPase pump
Give the mechanism of action of methylxanthines
Methylxanthines inhibit phosphodiesterase enzyme type 4 (PDE4). Leads to accumulation of intracellular cAMP and cGMP leading to bronchodilation
Inhibition of PDE4 reduces release of cytokines.
Improves skeletal muscle contractility
Adverse effects of thyophylline?
Gastrointestinal: nausea, anorexia, vomiting, abdominal pain, diarrhea, hyperacidity
Neurological: Headache, tremor, irritability, insomnia, confusion, dizziness, tinnitus, major seizures
Cardiovascular: Cardiac dysrhythmias
Allergic: Rashes, fever
Mechanism of action of corticosteroids?
Inhibition production of inflammatory cytokines IL 1, 2, 3, 4 TNF
Inhibition of phospholipase A2 which inhibition breakdown of arachidonic acid which all metabolic products of arachidonic acid as leukotrienes
Inhibition of eosinophilic and lymphatic airway mucosal inflammation of asthmatic airways
Inhibition of antibody formation
Increase B2 agonist action
Adverse of inhaled corticosteroids
Oropharyngeal candidiasis
Hoarseness of voice
Why ciclesonide is preferred than other lipid soluble corticosteroids?
enters small airways with high lung deposition. Is a prodrug activated by cleavage by esterases in bronchial epithelial cells. It causes less dysphonia and candidiasis than other corticosteroids
Give the reason mast cell stabilizers have little clinical use
Because cromolyn is not a bronchodilator, it is not useful managing an acute asthma attack. It also has short duration of action.
Enumerate the clinical use of mast cell stabilizers
Bronchial asthma
Allergic rhinitis
Allergic conjunctivitis
Give the clinical use of leukotrienes antagonist?
They are in benefit is asthma with concomitant allergic rhinitis
Enumerate the side effects of leukotrienes antagonist
Insomnia and irritability
Vivid dreams
Vasculitis
Eosinophilia
What are the indications of acetylcysteine?
Mucolytic adjuvant therapy for viscous secretions in acute and chronic pulmonary disease
Diagnostic bronchial studies
Acetaminophen antidote
Therapeutic uses of mucolytics?
In conditions like COPD and bronchial asthma
Cystic fibrosis
Bronchiectasis
Emphysema
Chronic bronchitis and chronic otitis media
Mechanism of action of Cimetidine
Selective competitive blocker of H2
Decrease Gastric acidity
Decrease formation of pepsin
Decrease secretion of intrinsic factor
Does not affect gut motility
Give the adverse affects of cimetidine?
Sudden stop–> ulcer and bleeding rehappens
GIT—> Constipation or diarrhea
Hypersensitivity–> skin rash
Decrease hepatic blood flow
Anti Androgen in males
increase prolactin in females
Explain; it is better to avoid clopidogrel with proton pump inhibitors
Clopidogrel is a prodrug that requires activation by the P450 enzyme, which is involved in metabolism of PPIs. PPIs could reduce clopidogrel activation.
What are the advantages and diff P-CAB over PPI?
They have faster onset of action and achieve rapid acid suppression at fist dose
Inhibit effect of H/K ATPase enzyme without need for activation
They bind to active and inactive forms of proton pump
Don’t require enteric coat
Give 4 adverse effects of proton pump inhibitor
Decrease bioavailability of vitamin B12 and digoxin
Long-term acid suppression leads to increased chronic inflammation in the gastric body
Decrease metabolism of Warfarin, Theophylline and Diazepam
CNS: Dizziness and drowsiness
Mechanism of action of Proton Pump Inhibitor?
It is a prodrug activates in acid environment
It is a irreversible inhibitor H/K ATPase enzyme
Decrease Basal and stimulated gastric acidity but no effect on GIT motility
Mechanism of action of metoclopramide as an anti-emetic?
Centrally blocks D2 receptor in CTZ
Peripherally–> Stimulates 5-HT4 receptors in enteric ganglia–> release of Ach—> increase gastric motility —> increase gastric emptying
Give an account on the mucosal protective PGE1-E2
Prevents NSAID induced gastric ulcer and promotes ulcer healing.
Increase HCO3, Mucus while decreasing HCL
Misoprostol is an example
SE: Diarrhea, colic
Give an account on the mucosal Sucralfate?
Increase mucus, PG. Decrease pepsin
SE: Constipation and decrease absorption
Gastrofate is an example
Give an account on the mucosal Colloidal Bismuth
Increase Mucus, PG, decrease pepsin. Bactericidal against H. Pylori
SE: black discoloration of stool and mouth
Carbenoxolone Na
Increase Mucus, PG
SE: Aldosterone like action
Biogastrone/ Liquorice roots
Give reason gastrofate “sucralfate” not given with H2 Blockers?
Because it acquires acid PH for activation
Mechanism of action of Metoclopramide “primperan”?
Antiemetic:
central: blocks D2-receptors in CTZ
Peripheral: stimulate 5-HT4 receptors in enteric ganglia–> release Ach–> Gastric motility–> increase gastric emptying–> prokinetic agent
Adverse affects of Metoclopramide “primperan”?
Dizziness
Nervousness
Parkinsonism
Ataxia
Hyperprolactinemia
Uses of Metoclopramide “primperan”?
All vomiting EXCEPT motion sickness
Gastric hypomotility
GERD
Hiccup
increase absorption of concomitantly drugs
Potassium-competitive acid blocker (P-CAB) side effects
Nausea, abdominal distention, diarrhoea
Risk of fracture
Hepatic function abnormalities
Hypersensitivity reaction
Domeperidone mechanism of action
CNS: blocks D2 receptor in CTZ
Peripherally–> gastric motility —> prokinetic
What are the disadvantages
Colic
Excreted in milk—> diarrhea in suckling baby
Excreted in urine—> red discoloration
Mechanism of action of leukotrienes
Zileuton is a 5 lipooxygenase inhibitor—> blocking leukotrienes synthesis
Zafirleukast and Montelukast are LTD4 receptor antagonist —–> Blocking LTD4 receptors
Bromhexine mechanism of action
Causes depolymerization of mucopolysaccharide of ground substance of sputum so they liquefy sputum.
Ambroxol mechanism of action
Ambroxol accumulates in lamellar bodies, secretory lysosomes of type II pneumocytes that store surfactant, where in affects hydrogen and calcium ion homeostasis leads to loss of lamella.
Acetylcysteine indication
Mucolytic adjuvant therapy for viscous secretions in acute and chronic pulmonary disease
Diagnostic bronchial studies
Acetaminophen antidote
Pharmacodynamics of Acetylcysteine
It splits disulfide bonds that are responsible for holding the mucous material together
This results in a decrease in the tenacity and viscosity of secretion.
