Pharma Topic List B Flashcards
B.3. Cholinomimetics - Drugs
carbachol
pilocarpine
neostigmine
pyridostigmine
rivastigmine
edrophonium
B.3. Cholinomimetics - Effects
i.e. parasympathomimetics – Rest and Digest
Eye - contraction of iris sphincter and ciliary m.
Salivary - inc secretion
Heart - inc vagal - negative chronotropy, dromotropy, inotropy
BV - dec BP - smooth muscle relaxation
Lungs - Bronchoconstriction
Stomach - inc gastric secretion
Intestine - inc motility
Urinary Tract - alleviate retention
B.3 Cholinmemtics - AChEi poisoning
DUMBBELS
D - diarrhea
U - urination
M - miosis
B - bradycardia
B - bronchoconstriction
E - excitation - CNS, muscles
L - lacrimation
S - secretion - sweating, salivation
carbachol
Is a synthetic choline ester
Direct acting cholinomemtic that is highly resistant to AchE hydrolysis
Acts on both N and M - not specific so rarely used
4˚ amine - no BBB
Topical - eyedrops
t1/2= 1 hr
tx: Acute Angle Glaucoma - opens canal of Schlemm
SE - CV and GI effect - stimulates and then depresses
N-R can cause release of E from adrenal medulla
B.3. Cholinomimetics
pilocarpine
Direct acting Cholinomimetic - Alkaloid so it is specific for muscarinic - Muscarinic Agonist
3˚ amine Yes BBB
Resistance to AchE hydrolysis
PO (eyedrops), Parentral
DoA - 30 min - 2h
Tx - Xerostoma from Sjøgren - systemic
DoC - glaucoma
OD- Antidote Atropine
B.3. Cholinomimetics
neostigmine
Indirect Acting Cholinomimetic
Non-competitive AchEi
4˚amine - no BBB
its a carbamate
main site of action is NMJ
IV - poor absorption in GI
tx: non-obstructive ileus, urinary retention
Used as an antidote for non-depolarizing curare like drugs post-op
CI - intestinal or urinary obstruction
B.3. Cholinomimetics
pyridostigmine
Indirect acting - Non-competitive AchEi
4˚amine - NO BBB
PO
DoA = 3-6hr
Main site of action - NMJ
tx: DoC for Myasthenia Gravis
paralytic ileus, urinary bladder atony
can be used against nerve gases
B.3. Cholinomimetics
rivastigmine
Non-Competitive AchEi - Indirect acting Cholinomemtic
Long acting t1/2 = ±70 hr
lipid soluble - YES BBB
hydrolyzed to carbamylated metabolite - no interactions
tx: transdermal patch - Alzheimer’s
first line drug with Donepezil, Galantamine
can delay the progession but cannot stop the disease
SE - GI distresss, cholinergic sym subside with continuing use
B.3. Cholinomimetics
edrophonium
Competitive AchEi
Short acting t1/2 = 5-15 mins with rapid renal elimination
to short for therapeutic use
PO
4˚amine - limited to periphery
Used: Tensilon test for diagnosis of Myasthenia Gravis
If too much given - antidote with atropine
B.3. Cholinomimetics
B.4. Muscarinic receptor blocking drugs
atropine
scopolamine
butyl-scopolamine
ipratropium
procyclidine
solifenacin
cyclopentolate
tiotropium
oxybutinine
atropine
B.4. Muscarinic receptor blocking drugs
scopolamine
B.4. Muscarinic receptor blocking drugs
butyl-scopolamine
B.4. Muscarinic receptor blocking drugs
ipratropium
B.4. Muscarinic receptor blocking drugs
procyclidine
B.4. Muscarinic receptor blocking drugs
solifenacin
B.4. Muscarinic receptor blocking drugs
cyclopentolate
B.4. Muscarinic receptor blocking drugs
tiotropium
B.4. Muscarinic receptor blocking drugs
oxybutinine
B.4. Muscarinic receptor blocking drugs
B.5. Catecholamines - Drugs
epinephrine
norepinephrine
dopamine
isoprenalin
dobutamine
epinephrine
B.5. Catecholamines
norepinephrine
B.5. Catecholamines
dopamine
B.5. Catecholamines
isoprenalin
B.5. Catecholamines
dobutamine
B.5. Catecholamines
B.6. Indirect sympathomimetics. Selective Alpha2-agonists and drugs acting on the imidazoline receptors - Drugs
ephedrine
phenylephrine
clonidin
rilmenidine
methyldopa
oxymetazoline
ephedrine
B.6. Indirect sympathomimetics. Selective Alpha2-agonists and drugs acting on the imidazoline receptors
phenylephrine
B.6. Indirect sympathomimetics. Selective Alpha2-agonists and drugs acting on the imidazoline receptors
clonidin
B.6. Indirect sympathomimetics. Selective Alpha2-agonists and drugs acting on the imidazoline receptors
rilmenidine
B.6. Indirect sympathomimetics. Selective Alpha2-agonists and drugs acting on the imidazoline receptors
methyldopa
B.6. Indirect sympathomimetics. Selective Alpha2-agonists and drugs acting on the imidazoline receptors
oxymetazoline
B.6. Indirect sympathomimetics. Selective Alpha2-agonists and drugs acting on the imidazoline receptors
B.7. alpha-receptor antagonists - Drugs
prazosin
doxazosin
tamsulozin
urapidil
carvedilol
phentolamine
prazosin
B.7. alpha-receptor antagonists
doxazosin
B.7. alpha-receptor antagonists
tamsulozin
B.7. alpha-receptor antagonists
urapidil
B.7. alpha-receptor antagonists
carvedilol
B.7. alpha-receptor antagonists
phentolamine
B.7. alpha-receptor antagonists
B.8. Beta-receptor antagonists - Drugs
propranolol
pindolol
carvedilol
timolol
sotalol
metoprolol
bisoprolol
nebivolol
esmolol
propranolol
B.8. Beta-receptor antagonists
pindolol
B.8. Beta-receptor antagonists
carvedilol
B.8. Beta-receptor antagonists
timolol
B.8. Beta-receptor antagonists
sotalol
B.8. Beta-receptor antagonists
metoprolol
B.8. Beta-receptor antagonists
bisoprolol
B.8. Beta-receptor antagonists
nebivolol
B.8. Beta-receptor antagonists
esmolol
B.8. Beta-receptor antagonists
B.9. Centrally acting skeletal muscle relaxants (spasmolytics). Dantrolene. Botulinum toxin - Drugs
baclofen
tolperisone
diazepam
tizanidine
dantrolene
botulinum toxin
baclofen
B.9. Centrally acting skeletal muscle relaxants (spasmolytics). Dantrolene. Botulinum toxin
tolperisone
B.9. Centrally acting skeletal muscle relaxants (spasmolytics). Dantrolene. Botulinum toxin
diazepam
B.9. Centrally acting skeletal muscle relaxants (spasmolytics). Dantrolene. Botulinum toxin
tizanidine
B.9. Centrally acting skeletal muscle relaxants (spasmolytics). Dantrolene. Botulinum toxin
dantrolene
B.9. Centrally acting skeletal muscle relaxants (spasmolytics). Dantrolene. Botulinum toxin
botulinum toxin
B.9. Centrally acting skeletal muscle relaxants (spasmolytics). Dantrolene. Botulinum toxin
B.10. Skeletal muscle relaxants acting on the neuromuscular junction - Drugs
atracurium
cisatracurium
mivacurium
pipecuronium
rocuronium
succynylcholine (suxamethonium)
atracurium
B.10. Skeletal muscle relaxants acting on the neuromuscular junction
cisatracurium
B.10. Skeletal muscle relaxants acting on the neuromuscular junction
mivacurium
B.10. Skeletal muscle relaxants acting on the neuromuscular junction
pipecuronium
B.10. Skeletal muscle relaxants acting on the neuromuscular junction
rocuronium
B.10. Skeletal muscle relaxants acting on the neuromuscular junction
succynylcholine (suxamethonium)
B.10. Skeletal muscle relaxants acting on the neuromuscular junction
B.11. Selective Beta2-stimulants and other bronchodilators. Pharmacotherapy of bronchial asthma and COPD. - Drugs
salbutamol
terbutaline
fenoterol
salmeterol
formoterol
ipratropium
tiotropium
theophyllin
B.11. Selective Beta2-stimulants and other bronchodilators. Pharmacotherapy of bronchial asthma and COPD. - Pharma of Bronchial Asthma
chronic inflam disease of airways with bronchoconstriction, dyspnea, cough, chest rightness, wheezing.
Goal of tx – reduce intensity and frequency of sympt and limitation caused by them.
Quick relief, long term – reverse and prevent airway inflam.
Steps to tx –
1. Assess severity and start tx accord to guideline.
2. Inc intensity of tx stepwise until well controlled
3. Dec dose of anti-inflam gradually.
1st stage – mild – SABA inhaler, or anitmusc inhal or oral SABA – symps 1x week, nighttime 2x/month FEV1>80%.
2nd stage – mild, persistent – reliever + small dose steroid inhaler or leukotriene inhib – symp 2x/week more than 2x night and FEV1>80%.
3rd stage – moderate, persistent. Reliever+small dose steroid+LABA – daily symp and FEV1 60-80%. 4th stage – severe and persistent. Reliever+med/high dose steroid +LABA.
B.11. Selective Beta2-stimulants and other bronchodilators. Pharmacotherapy of bronchial asthma and COPD. - Pharma of COPD
chronic irreversible obstruction of airflow that is progressive.
Tx depends on patient category.
A – SAMA/SABA can add LABA or theophylline.
B – LAMA/LABA can add SABA or theophylline.
C-ICS+LABA can add PDE4 inhibitor or theophylline.
D – ICS+LABA can add PDE4i, carbocysteine or theophylline.
ICS inhaled corticosteroids
salbutamol
Short acting beta2 agonist – Gs – inc [cAMP] – smooth m relax – bronchodilation
T1/2 – 4 hr, OoA 5 min. aerosol, nebulizer, parenteral.
TX – asthma, COPD, no prophylaxis. SE – tachycardia, tremor, arrhythmia
B.11. Selective Beta2-stimulants and other bronchodilators. Pharmacotherapy of bronchial asthma and COPD.
terbutaline
Short acting beta2 agonist – Gs – inc [cAMP] – smooth m relax – bronchodilation
T1/2 – 4 hr, OoA 5 min. aerosol, nebulizer, parenteral.
TX – asthma, COPD, no prophylaxis. SE – tachycardia, tremor, arrhythmia
B.11. Selective Beta2-stimulants and other bronchodilators. Pharmacotherapy of bronchial asthma and COPD.
fenoterol
Short acting beta2 agonist – Gs – inc [cAMP] – smooth m relax – bronchodilation
T1/2 – 4 hr, OoA 5 min. aerosol, nebulizer, parenteral.
TX – asthma, COPD, no prophylaxis. SE – tachycardia, tremor, arrhythmia
B.11. Selective Beta2-stimulants and other bronchodilators. Pharmacotherapy of bronchial asthma and COPD.
salmeterol
Long acting beta2 agonist.
DoA 12-24 hr.
PO, aerosol, nebulizer, parenteral.
TX – bronchodilation in asthma, COPD, prophylaxis – beneficial when used with corticosteroids.
SE – tachycardia, tremor, arrythmia
B.11. Selective Beta2-stimulants and other bronchodilators. Pharmacotherapy of bronchial asthma and COPD.
formoterol
Long acting beta2 agonist.
DoA 12-24 hr.
PO, aerosol, nebulizer, parenteral.
TX – bronchodilation in asthma, COPD, prophylaxis – beneficial when used with corticosteroids.
SE – tachycardia, tremor, arrythmia
B.11. Selective Beta2-stimulants and other bronchodilators. Pharmacotherapy of bronchial asthma and COPD.
ipratropium
SAMA – muscarinic antagonist. Competitive inhibitor of M3R (Gq) – prevents bronchoconstriction mediated by vagal discharge.
Aerosol.
Onset <15 min DoA 4-6h – admin 3/day.
TX – asthma, COPD – beneficial for patients with cardiac disease.
SE – dry mouth, cough
B.11. Selective Beta2-stimulants and other bronchodilators. Pharmacotherapy of bronchial asthma and COPD.
tiotropium
LAMA – M3 antagonist. Aerosol. Longer acting.
TX – asthma, COPD
B.11. Selective Beta2-stimulants and other bronchodilators. Pharmacotherapy of bronchial asthma and COPD.
theophyllin
PDE3 inhibitor – prevents the breakdown of cAMP – inc cAMP in smooth muscle cells leading to bronchodilation.
Methylaxanthine derivative.
PO, slow release.
DOA 12 hr. hepatic CYP450.
TX – asthma – prophylaxis in nocturnal attacks, AHF, anti-inflamm.
SE – GI distress, insomnia, tremor, anorexia, seizures, cardiac stimulation chon and ino, arrythmia, CNS
B.11. Selective Beta2-stimulants and other bronchodilators. Pharmacotherapy of bronchial asthma and COPD.
B.12. Antiinflammatory agents used in bronchial asthma. Antitussive agents and expectorants - Drugs
prednisolone
methylprednisolon
fluticazone
budesonide
montelukast
omalizumab
codein
butamirate
prenoxdiazine
acetylcystein
bromhexin
prednisolone
inhaled GC.
TX – severe asthma – can use systemic PO.
Most effective anti-inflam agent used in asthma.
Inhibits PLA2 – dec COX – dec inflame mediators, dec inflame cells in airway, dec eosinophils dec activated T cells and mast cells.
Inc beta-2 R expression.
SE – infection – oral candiasis, hyperglycemia, Cushings
B.12. Antiinflammatory agents used in bronchial asthma. Antitussive agents and expectorants
methylprednisolon
inhaled GC.
TX – severe asthma – can use systemic PO.
Most effective anti-inflam agent used in asthma.
Inhibits PLA2 – dec COX – dec inflame mediators, dec inflame cells in airway, dec eosinophils dec activated T cells and mast cells.
Inc beta-2 R expression.
SE – infection – oral candiasis, hyperglycemia, Cushings
B.12. Antiinflammatory agents used in bronchial asthma. Antitussive agents and expectorants
fluticazone
inhaled GC for asthma and COPD
B.12. Antiinflammatory agents used in bronchial asthma. Antitussive agents and expectorants
budesonide
Topical GC tx bronchial asthma, allergic rhinitis. Enema- IBD
B.12. Antiinflammatory agents used in bronchial asthma. Antitussive agents and expectorants
montelukast
selective antagonist of CysLT1 Receptor which dec LDT4 (leukotriene D4).
Prevents Leukotrienes binding to receptor – dec bronchoconstriction and inflamm.
Smooth muscle relaxant.
TX – exercise induced asthma, long term maintenance.
SE – upper resp infect, headache, fever.
B.12. Antiinflammatory agents used in bronchial asthma. Antitussive agents and expectorants
omalizumab
(humanized) – Anti-IgE antibody.
Binds the Fc portion of the IgE Ab – binding to high affinity R on mast cells is prevented – dec inflamm response to inhaled antigens.
EXPENSIVE. Parenteral.
TX – prophylaxis of severe refractory asthma, that doesn’t respond to other drugs
B.12. Antiinflammatory agents used in bronchial asthma. Antitussive agents and expectorants
codein
mu opioid R agonist.
Antitussive, analgesic effect.
Weak semi-synthetic morphine agonist – suppresses cough reflex. 10% of codeine is transformed into morphine by CYP2D6.
SE – constipation, dependence
B.12. Antiinflammatory agents used in bronchial asthma. Antitussive agents and expectorants
butamirate
non-opioid centrally acting antitussive – suppresses cough reflex. PO.
Peripheral effect – bronchodilation, suppress inflamm. TX – cough
B.12. Antiinflammatory agents used in bronchial asthma. Antitussive agents and expectorants
prenoxdiazine
antitussive that acts on periphery. Dec receptor sensitivity, dec sensitivity of afferent nerves, inhibit cough reflex.
Works as local anesthetic in bronchoscopy.
B.12. Antiinflammatory agents used in bronchial asthma. Antitussive agents and expectorants
acetylcystein
mucolytic expectorant. Cleaves mucopolysacc and glucopro of mucus – diluting the mucus and dec viscosity.
Has thiol group – cleaves disulfide bridges.
TX – CF, chronic bronchitis, bronchiectasis.
B.12. Antiinflammatory agents used in bronchial asthma. Antitussive agents and expectorants
bromhexin
mucolytic expectorant. Inc the production of serous fluid in the resp tract, which makes phlegm thinner. PO
TX – CF, chronic bronchitis, bronchiectasis
B.12. Antiinflammatory agents used in bronchial asthma. Antitussive agents and expectorants
B.13. Drugs used for the treatment of peripheral vascular diseases. Therapy of migraine - Drugs
vinpocetin
nicergolin
cilostazol
pentoxifyllin
Ca-dobesilate
sumatriptan
galkanezumab
cinnarizin
propranolol
verapamil
carbamazepine
valproate
imipramine
vinpocetin
B.13. Drugs used for the treatment of peripheral vascular diseases. Therapy of migraine
nicergolin
B.13. Drugs used for the treatment of peripheral vascular diseases. Therapy of migraine
cilostazol
B.13. Drugs used for the treatment of peripheral vascular diseases. Therapy of migraine
pentoxifyllin
B.13. Drugs used for the treatment of peripheral vascular diseases. Therapy of migraine
Ca-dobesilate
B.13. Drugs used for the treatment of peripheral vascular diseases. Therapy of migraine
sumatriptan
B.13. Drugs used for the treatment of peripheral vascular diseases. Therapy of migraine
galkanezumab
B.13. Drugs used for the treatment of peripheral vascular diseases. Therapy of migraine
cinnarizin
B.13. Drugs used for the treatment of peripheral vascular diseases. Therapy of migraine
propranolol
B.13. Drugs used for the treatment of peripheral vascular diseases. Therapy of migraine
verapamil
B.13. Drugs used for the treatment of peripheral vascular diseases. Therapy of migraine
carbamazepine
B.13. Drugs used for the treatment of peripheral vascular diseases. Therapy of migraine
valproate
B.13. Drugs used for the treatment of peripheral vascular diseases. Therapy of migraine
imipramine
B.13. Drugs used for the treatment of peripheral vascular diseases. Therapy of migraine
B.14. Drugs used for treatment of heart failure I: Drugs decreasing the load on the heart. Drugs of acute cardiac failure. Pharmacotherapy of chronic heart failure. - drugs
ACE-inhibitors, diuretics, beta-blockers
B.15. Drugs used for treatment of heart failure II: Positive inotropic agents. Pharmacotherapy of acute heart failure. - Drugs
digoxin
digitoxin
milrinone
levosimendan
dobutamine
digoxin
B.15. Drugs used for treatment of heart failure II: Positive inotropic agents. Pharmacotherapy of acute heart failure
digitoxin
B.15. Drugs used for treatment of heart failure II: Positive inotropic agents. Pharmacotherapy of acute heart failure
milrinone
B.15. Drugs used for treatment of heart failure II: Positive inotropic agents. Pharmacotherapy of acute heart failure
levosimendan
B.15. Drugs used for treatment of heart failure II: Positive inotropic agents. Pharmacotherapy of acute heart failure
dobutamine
B.15. Drugs used for treatment of heart failure II: Positive inotropic agents. Pharmacotherapy of acute heart failure
B.16. Antiarrhytmic agents - Drugs
lidocaine
propafenone
esmolol
amiodarone
sotalol
verapamil
adenozine
digoxin
Mg++
lidocaine
B.16. Antiarrhytmic agents
propafenone
B.16. Antiarrhytmic agents