Pharmacology Terms (drugs, etc.)
Terms
undefined, object
copy deck
- Zileuton
- 5-LOX inhibitor (for ashtma)
- zafirlukast
- LTD4, LTE4 antag
- methylxanthines
-
- for asthma (bronchodilator) by:
- block adenosine
- inhibit phosphodiesterase
- other effects like caffeine (since caffeine is one... incr. HR, incr. alert, incr. gastric acid + pepsin, conulsions and arrhythmia at high doses, etc.)
- removed by CYP 450 in liver; drug interactions bad because low therapeutic range - xanthine oxidase
- - makes uric acid (gout)
- diphenhydramine
-
- H1 antag (1st gen)
- dry mouth (anticholinergic) - phenothiazines
-
- H1 antag (1st gen)
- also block seretonin and Epinephrine - chlorpheniramine (like diphenhydramine))
- - H1 antag (1st gen)
- Loratidine
- - H1 antag (2nd gen)
- cetirizine
- H1 antag (2nd gen)
- dimenhydrinate
- - gravol (h1 antag)
- cimetidine
-
- H2 antag
- inhibits CYP P450 - ranitidine
- - H2 antag
- famotidine
- - H2 antag
- serotonin is made from what aa?
- tryptophan
- NE and E made from which aa?
- tyrosine
- enterochromaffin-like cells hold what?
- histamine
- enterochromaffin cells hold what?
- serotonin
- sumatriptan
- 5HT1 agonist (for migrane)
- Ondansetron
- - 5HT3 antag (antiemetic)
- cisapride
-
(hard)
- 5HT4 agonist (incr. GI motility) - tubocurarine
-
- displaces histamine from heparin binding sites in granules, along with morphine
- neuro muscular inhibitor - cromolyn
- stop mast degranulation
- urticaria
- hives
- bromocriptine
-
- stimulates dopamine / dopamine agonist
- inhibits prolactin - dopamine inhibits what hormone?
- prolactin
- ergot alkaloids are agonists for what receptors?
- 5HT, dopamine, alpha
- SRS-A contains what?
-
- slow reacting substances of anaphylaxis
- LTC4, E4, D4 - indomethacin
-
- indole derivative
- potent cyclooxygenase inhibitor
- lots toxicities to it (headache, nausea, psychoses, ulcers, thrombocytopenia, aplastic anemia, confusion, depression)
- (used to close ductus arteriosus) - misoprostol
-
- PGE analog
- stop stomach secretions (acid, etc.)
- give with arthritis drugs (when inhibit PG) so won't get ulcers
- causes diarrhea - leuteolytic effect
- - regression of corpeus leutium (from PGF2a effects)
- glucocorticoid
-
- stimulate synthesis lipocortin -> inhibit phospholipase
- decrease AA -> decrease eicosenoids - lipocortin
-
- stimulated by glucocorticoid
- inhibit phospholipase (therefore AA) - celecoxib
- celebrex (cox II inhib)
- rofecoxib
- vioxx (cox II inhib)
- ETYA
-
- like AA, but triple bonds (so inhibit lipooxygenase, maybe cyclo too?)
- lipid soluble, so sucked up into random places, doesn't work in vivo - FLAP
- 5-lipooxygenase activating protein
- montelukast
-
(hard)
Leukotriene inhibitor
- tradename singulair - ASA is bad for people with what 3 conditions?
-
- ulcers (because incr. acid in stomach)
- asthma (bronchconstriction, etc.)
- renal failure (PG reliant) - aryl propionic acid derivatives
- NSAIDs like ibuprofin, naproxin
- naproxin
- like ibuprofin, but t1/2 = 14h instead of 2-6
- DMARDs
-
Disease Modifying Anti Rhumetic Drugs
(aka - SAARDs - slow acting...) - hydroxychloroquine
-
- a DMARD
- antimalarial
- ototoxicity and ocular toxicitity (retinopathy) - teratogenicity
- - birth defects
- stomatitis
- swelling of oral mucosa
- methotrexate
-
immunosuppressive drug (a DMARDs)
- causes stomatitis, teratogenicity, and GI defects - TNF-a
- proinflammatory cytokine
- IL-1
- proinflammatory cytokine
- infliximab
- monoclonal antibody to TNFa
- etanercept
-
- bind 2 TNFa
- increase chance Tb - sodium urate crystals are the problem in...
- gout
- colchicine
-
- stop migration of MTs in granulocytes, inhibiting migration
- for gout - allopurinol
-
- inhibit Xanthine Oxidase
- forms alloxanthine, which also inhibits - uricosuric drugs
- - decrease urate reabsorption in proximal tuble (for gout)
- probenecid
- uricosuric drug
- sulfinpyrazone
- uricosuric drug
- acute (stopping of asthma)
- termination of attack
- prophylactic (stopping of asthma)
- prevention of attack
- sodium cromoglycate (cromolyn sodium)
-
stops mast cell degranulation (asthma)
- with inhaler - beclomethasone
- - a glucocorticoid (for asthma)
- theophylline
-
- a methylxanthine (the prototype)
- others are caffeine and theobromine - treatment for infantile apnea
- methylxanthines
- PSNS predominates: (4 items)
-
- cilliary muscles
- heart
- salivary glands
- bronchiole smooth muscle - SNS predominates: (2 items)
-
- sweat glands
- veins and arterioles - sweat glands have what type of receptor?
- muscarinic (even though SNS)
- renal vascular smooth muscle has what type of receptor?
- dopamine (even though SNS)
- hemicholinium
- stops uptake of choline (with Na)
- choline acetyl transferase
- makes ACh from choline and AcCoa
- vesamicol
- inhibits transport of ACh into vesicles
- tyrosine hydroxylase
-
- tyrosine -> DOPA
- rate limiting step of NE formation - aromatic a.a. decarboxylase
- DOPA -> dopamine
- dopamine-B hydroxylase
-
- dopamine -> NE
- in vesicle - metyrosine
- inhibit tyrosine hydroxylase
- PNMT
- NE -> E (in adrenal medulla)
- reserpine
- - stops transfer of dopamine into vesicles (for NE)
- cocaine
- - inhibit reputake of NE
- COMT
-
- catechol-o-methyltransferase
- metabolise NE - MAO
-
monoamine oxidase
- metabolise NE - atropine
- block muscarinic
- adrenal medulla has what type of receptor?
- Nn
- M1 + M3 acts through what second messenger?
-
- incr. IP3, DAG
- incr. CA, activ. PKC - M2 acts through what second messenger?
-
- decr. adenylyl cyclase
- decr. CA, open K+ - a1 acts through what second messenger?
-
- incr. IP3, DAG
- incr. CA, activ. PKC - a2 acts through what second messenger?
-
- decr. adenylyl cyclase
- decr. cAMP dependent PK - B1 + B2 act through what second messenger?
-
- incr. adenylyl cyclase
- incr. cAMP dependent PK - baroreceptor reflex originates in the...
- carotid sinus (and aaortic arch)
- phenelzine
- MAO inhibitor
- mydriasis
- - pupil dilation
- what SNS receptor controls pupil size?
- a1 - contraction of radial pupillary dilatior
- what SNS receptor controls ciliary muscle?
- b2 - relaxes it
- what SNS receptor controls the liver?
- B2 - glyconeolysis, gluconeogenesis
- what SNS receptor controls the pancreas?
- a
- what SNS receptor controls fat cells?
- B1
- ipratropium
-
- like atropine
- synthetic, quaternary
- muscarinc blocker
- used for asthma (inhibit bronchoconstrict and secretions) - salbutamol
-
B2 agonist (for asthma)
- with inhaler
- salmeterol (longer acting) - tocolytic
- - stops premature labour
- phenylephrine
- - a1 + a2 agonist
- clondine
- - a2 agonist (for hypertension)
- dobutamine
- - b1 agonist (for failing heart)
- terbutaline
- - B2 agonist (prevent premature labour)
- ephedrine
-
- like amphetamine (release NE)
- used in China
- weak base, excreted in urine
- crosses BBB easily - methylphenidate
-
- like amphetamine
- for ADHD - tyramine
-
- amphetamine like
- cheese reaction (with MAO inhibitor) - pheochromocytoma
-
- catecholeamine secreting tumour of chromaffin tissue (hypertension)
- treat with a and b blockers - phenoxybenzamine
- - a1 + a2 antagonist (irreversable)
- phentolamine
- - a1 + a2 antagonist (competitive)
- yohimbine
- - a2 antag
- - Benign prostatic hypertrophy (BPH)
- - use a1 antag
- prazosin
- - a1 antag (to treat BPH)
- tamusolin
- - a1 antag
- atenolol / metoprolol
- - B1 antag
- miosis
- - contraction of pupils
- bethanechol
-
- M3 (and little M2) agonist
- GI motility
- bladder emptying - pilocarpene
-
- M3 agonist
- lipid soluble (3o amine)
- for glaucoma - butyrylcholinesterase
-
- plasma cholinesterase (+ liver, non-neuronal cells)
- hydrolyzes ester containing drugs - myasthenia gravis
-
- loss of N receptors
- muscle weakness; drooping eyelids, etc. - edrophonium
-
- reversible, short acting anticholinesterase
- not well absorbed
- diagnose myasthenia gravis - neostigmine
-
- reversible, medium acting anticholinesterase
- not well absorbed
- treat myasthenia gravis
- anesthtists reverse NMJ blocking drugs
- incr. GI motility, empty bladder - physostigmine
-
- reversible, mid acting anticholinesterase
- well absorbed
- treat glaucoma topically - parathion
-
- permanent cholinesterase blocker
- insectiside
- toxic humans - can't remove - malathion
-
- permanent cholinesterase blocker
- insectiside - ecothiophate
-
- permanent cholinesterase blocker
- not well absorbed
- treat glaucoma topically - sarin
-
- permanent cholinesterase blocker
- used in war - alzheimer's is trying what as a drug?
- cholinesterase inhibitors
- pralidoxime
- cholinesterase reactivator
- cycloplegia
- - no near vision (when you have muscarinic blockers)
- muscarinic antag do what to HR?
-
- first decr. (because loss of negative feedback)
- then incr. - scopolamine
- - muscarinic antagonist (lipid soluble)
- lobeline
-
- like nicotine, less potent
- lipid soluble
- both are alkaloids (acidic urine makes excretion easier) - trimethaphan
-
- ganglionic blocking drug
- used for hypotension in certain anesthetic procedures - hexamethonium
-
- ganglionic blocking drug
- originally used for hypotension - pancuronium
- - neuromuscular blocking agent (longest lasting)
- vecuronium
- - neuromuscular blocking agent (shortest and fastest)
- decamethonium
-
depolarizing neuromuscular blocking agent
- not succeptable to cholinesterase - succinylcholine
- - depolarizing neuromuscular blocking agent
- Reyes syndrome
-
- neurological disorder
- happens when give ASA to kids with fever - tartazine
-
- yellow food colouring
- allergic to ASA of allergic to this - capsicum
-
- heat in heat rubs
- in hot peppers - pseudoephedrine
- - a agonist (used in cold preparations as decongestant)
- phenylpropanolamine
-
- a agonist (for decongestant)
- not used anymore because caused strokes in young women - dextromethorphan
-
- cough suppressent
- codeine also works - glyceryl guaiacolate
- - an expectorant (in cold medication)
- expectorant
- - reduce viscosity of septum (supposed to...)
- antiseptic
-
- kills bacteria
- in lozenges / mouthwash
- phenols, benzoic acid, cetylpyridinium chloride - hydrocortisone
-
- reduce inflammation
- for poison ivy, insect bites - calamine lotion
-
- for insect bites, poison ivy
- cooling, temporary relief - valerian
-
- contain valepotriates
- "sedative and hypnotic" (CNS depressant, so interaction with alcohol?)
- placebo - Devil's Claw
-
- for inflammation
- biotransformmed in gut -> not effective - comefrey
-
- stimulates cell proliferation
- wound healing
- should not be used internally -> liver injury (people use for ulcers though) - feverfew
-
- for migranes
- lots of toxicities
- antipyretic, antispasmodic, emmenogogue
- - sesquiterpene lactones (in what herbal?)
-
(hard)
- in feverfew - ginseng
-
- adaptogen
- aphrodesiac
- enhances memory, learning, physical stamina, health
- yeah right! - kava
-
- anti-anxiety
- mild sedative
- problems with alcohol, scaly skin... severe warnings from health canada - warfarin
- - anticoagulant
- thalidomide
-
- prevent morning sickness
- in first trimester, has teratogenicity on child - cabachol
-
- like Ach
- less succeptable to AchE - methacholine
-
- like Ach
- a bit less Nicotinic activity
- a bit less AchE activity - bromfenac
- - NSAID taken off market because of serious hepatotoxicity
- carbamazepine
-
- anticonvulsant
- serious hypersensitivity reactions - hapten
- - drug that binds to protein, then can be sensitzed to it (allergic response)
- clavulinic acid
- - increases effects of penicillin
- sulfonamides
- - displace methotrexate, phenytoin, and warfarin from albumin (therefore, higher blood conc.)
- ethanol, carbamazepine, phenytoin - worry about what when taking these drugs?
- incr. effect CYP 450
- tetracycline
-
- antibiotic used for acne
- can't absorb when complex with antacid or Ca - debrisoquine hydroxylase deficiency
-
CYP 450 2D6 deficiency
- 2D6 metabolizes ecstacy, codeine - S-mephenytoin hydroxylase deficiency
- CYP 450 2C19 deficiency (Japanese and Chinese)
- NAT (2 types)
-
N acetyl transferase (Phase 2 rxn)
- NAT1 - broad, in lots tissues
- NAT2 - in specific tissues - isoniazid
-
- acetylated by NAT
- VB6 deficency when not enough NAT (neuronal toxicity) - thymidylate synthase
-
dUMP -> dTMP for DNA
- polymorphic - people with 3 (instead of 2) less effective anti-cancer drug - malignant hyperthemia
-
- when give anesthetic and depolarizing muscle relaxant
- Ca channel problem (stays open to stimulation)
- RYR1 gene - problem in pigs, 50% problem in humans - dimercaprol (BAL)
-
- chelating agent for bismuth, arsenic, lead, polonium, mercury
- DMSA less toxic (since BAL also toxic) - EDTA
-
- binds calcium, but lead much better
- chelating agent - oral penicillamine (chealating agent for...)
- for copper
- deferoxamine
- chealating agnet for iron
- CN (binds with? to treat (2 ways))
-
ferric iron (Fe3+) - use nitrile
- thiosulfate acts as sulfur source to inactivate - fomepizole
- - new alcohol dehydrogenaze inhibitor
- to treat bromide poisoning...
- give chlorine
- methylene blue
-
- to treat methemoglobinemia
- intermediate electron acceptor from NADPH