-
Theophylline MOA
- PDEase inhibitors; prevents breakdown of CAMP into 5'AMP
- Antagonizes adenosine receptors
-
Theophylline therapeutic uses
asthma
-
Caffeine MOA
- PDEase inhibitor, promotes wakefulness
- antagonizes adenosine A1 and A2
-
Caffeine effects
wakefulness
-
Caffeine uses
wakefulness
-
Sildenafil MOA
inhibits phosphodiesterase type 5, enhancing effects of nitric oxide-activated increases in cGMP
-
Sildenafil therapeutic uses
- relaxes mm and inc BF to particular areas of the body (viagra)
- ED
- Revatio: rx pulm art hypertension and improve exercise capacity in men and women.
-
Papaverine
PDEase inhibitor
-
Acetazolamide MOA
carbonic anhydrase inhib (makes urine more basic to increase excretion of WA like aspirin)
-
Acetazolamide uses
CHF, altitude sickness, glaucoma, seizure disorders
-
Ammonium chloride MOA
makes urine more acidic to inc excretion of WB like amphetamine
-
Acetylcholine
cholinergic agonists
-
methacholine
cholinergic agonist
-
carbachol (carbamycholine)
cholinergic agonist
-
bethanechol
cholinergic agonist
-
succinylcholine
cholinergic agonist
-
pilocarpine
cholinergic agonist
-
Phenobarbital
- induces CYP1A2, 2C, 3A4 (when you induce CYP450 isozymes, then drug effect is diminished bc there is more metab of the drug and more plasma Cl due to more active CYP450)
- pharmokinetic tolerance
-
-
Furanocoumarin
- inhibits CYP1A2, 3A4 (inc drug effect bc dec hepatic Cl)
- drug toxicity
-
Phenobarbital MOA
alters sensory cortex, cerebellar, and motor activities; produces sedation, hypnosis, and anesthesia (barbiturate)
-
Phenobarbital uses
- sedative
- treat/prevent seizures
- short term insomnia rx
-
Phenytoin
stimulates synth of CYP450
-
Ethanol
stim synth of CYP450
-
Dioxin
stim synth of CYP450
-
PCBs
stim synth of CYP450
-
Rifampin
(TB rx) stim synth CYP450
-
Carbamezpine
stim synth CYP450
-
cigarette smoke
stim synth CYP450
-
-
Cimetidine
inhib synth of CYP450
-
Isoniazid
(TB rx) inhib synth of CYP450
-
Ethanol (acute)
inhib synth of CYP450
-
Ketoconazole
(fungal rx) inhib synth CYP450
-
Erythromycin
inhib synth CYP450
-
Hemicholinium
blcoks choline uptake so that Ach synthesis is blocked
-
Opiates
inhibit Ach release in GI
-
Serotonin
Amplifies release of Ach in GI
-
Botunlinim toxin MOA
binds to surface proteins and its light chain shows protease activity to cleave proteins used in storage and therefore release Ach-->cholinergic nt will stop and result in mm paralysis
-
Botulinim Uses
- blephoraspasm
- strabismus
- cervical dystonia
- laryngela dystonia
- spasmodic torticollis
- myofascial pain syndrome
- hemifacial spasm
-
Tetanus toxin MOA
acts in conjunction w/ spinal cord to prevent release of inhib nt and results in spastic paralysis
-
Black widow spider toxin (alpha latrotoxin)
releases lots of Ach by binding to neurexins in PM
-
Neogstigmine
Inhibits Achase: slowly reversible carbamate inhibitor
-
Malathion
irreversible organophosphate inhib of Achase
-
Carbachol
agonist of nicotinic and muscarinic receptors
-
Carbachol uses
causes miosis after surgery in anterior chamber of the eye
-
Methacholine
- provocholine
- muscarinic agonist
-
Methacholine uses
proactive agent in dx of bronchial asthma
-
Bethanechol
- urecholine
- muscarinic agonist w/ selective action on GI and GU
-
Bethanechol Uses
Rx bowel stasis, postoperative paralytic ileus, urinary retention
-
Bethanechol CI
CHF, hyperthyroidism, asthma, COPD, peptic ulcers
-
Succinylcholine
- cholinergic receptor agonist
- IV: initial skel mm contraction then flaccid paralysis for 3-5min from constant depolarization of MEP (uses non competitive blocking of Ach)
-
Succinylcholine Termination
Determined by concentration of plasma cholinesterase before even at NMJ; diffusion away from NMJ determines true termination
-
Pilocarpine
- selective muscarinic agonist
- Pilocar, Isopto Carpine
-
Pilocarpine Uses
rx of glaucoma, dry mouth from Sjorgren's
-
Pilocarpine Terminatino
Degraded by hepatic enz and not metabolized by Achase or pseudocholinesterase
-
Cevimelline
- Evoxac
- synthetic muscarinic agonist
-
Pilocarpine and Glaucoma MOA
- muscarinic receptor agonist
- contracts meridional fibers of ciliary mm-->increases iridocorneal angle and/or tone and alignment of slots-->more aqueous humor now flows through Schlemm
-
Pilocarpine and glaucoma pharm effects
- IOP decreases by 20% w/ persistent miosis that will give poor night vision
- Contraction of ciliary mm gives fixation of lens for near vision so far vision impaired
-
Betaxolol MOA
- beta adrenoceptor antagonist
- Betaoptic
- selectively blocks B1 receptors to decrease secretion of aqueous humor
-
Betaxolol pharm effects
- lowers IOP by 20-30%
- bradycardia if any systemic absorption happens
-
-
Timolol MOA
- Beta adrenoreceptor antagonist
- timoptic
- decreases secretion of aquesous humor since it blocks beta
-
Timolol pharm effect
- lowers IOP by 20-30%
- bronchoconstriction and bradycardia if any systemic absorption happens
-
-
Latanoprost MOA
Analog of PGF2
-
Latanoprost pharm effect
- inc aqueous humor outflow
- lowers IOP by 20-25%
-
Latanoprost uses
glaucoma
-
Bimatoprost Uses
glaucoma
-
Bimatoprost MOA
PGF2 analog, prolongs eye lash growth
-
bimatoprost pharm effects
inc length and thickness of eyelashes
-
Epinepherin (glaucoma) MOA
- glaucon, epitrate
- <1% concentration: results in A2 stim-->dec synth of aq humor
- >1% concentration: results in A1 stim--> inc normal outflow of aq humor
-
Epinepherin Pharm effects
either inc outflow of aq humor or dec its secretion; conc dependent
causes mydriasis from stimulation of A1 in radial mm of iris
-
Apraclonidine MOA
stimulates A receptors
-
Apraclonidine pharm effects
reduces amt of aq humor to decrease IOP
-
Apraclonidine Uses
to decrease IOP after surgery
-
Acetazolamide MOA
- Diamox
- carbonic anhydrase inhibitor on ciliary epithelium
-
Acetazolamide pharm effect
decreases production of aq humor
-
Acetazolamide Uses
to decrease IOP, glaucoma
-
Dorzolamide MOA
- Trusopt
- carbonic anhydrase inhibitor on ciliary epithelium
-
Dorzolamide pharm effect
- dec IOP by 10-20%
- decrease production of aq humor
-
Dorzolamide Uses
glaucoma, lower IOP
-
Isofluophate (DFP) MOA
Decreases amt of Ach available to contract meridional fibers of ciliary mm
-
Isofluophate pharm effects
lowers IOP
-
Isofluophate uses
glaucoma
-
Isofluophate AE
toxicity and cataracts possible so only use on a pt if nothing else is working
-
Echothiophate MOA
binds irreversibly to Ach site on pseudoacetylcholinesterase (organophosphate cholinesterase inhibitor)
-
Echothiophate uses
glaucoma
-
Mannitol MOA
- osmitrol
- osmotic diuetic agent (elevates glomerular filtrate osmolarity)
-
Mannitol Uses
kidney failure (diuretic), dec IOP and brain P/swelling
-
Mannitol pharm effects
hyperosmolarity which leads to cellular dehydration and decreased IOP
-
Mannitol uses
angle-closure glaucomas
-
Memantine MOA
- Namenda
- binds N-methyl-D-aspartate receptors, may slow Ca++ influx and nerve damage (NMDA receptor antagonist)
- Note: prevents excitotoxicity and neuronal cell death (too much glutamate stimulation at NMDA receptors is bad but this prevents it)
-
Memantine Uses
Alzheimer's
-
Physostigmine MOA
- Synapton
- carbamate Achase inhibitor
-
Physostigmine AE
TOO MANY
-
Physostigmine Uses
Alzheimer's
-
Donepezil MOA
- Aricept
- carbamate Achase inhibitor
- DRUG OF CHOICE
-
Donepezil AE
decreased apathy, hallucinations, anxiety, behavior prob, n/v, diarrhea, mm cramps, fatigue, peeing, bradycardia, anorexia, syncope, insomnia, vivid dreams
-
Rivastigmine MOA
- Exelon
- carbamate Achase inhibitor
-
Rivastigmine uses
alzheimer's
-
Galantamine
- razadyne
- carbamate Achase inhibitor
-
Galantamine Uses
alzheimer's
-
Edrophonium MOA
- tensilon
- carbamate AChase inhibitor; only acts at NMJ via direct stimulation of cholinergic N2 receptors
-
Edrophonium Uses
- MG
- distinguish btw MG and cholinergic crisis
- reverse mm paralysis from competive nm blocking agents (like D-tubocurarine)
-
Neostigmine MOA
- prostigmin
- carbamate Achase inhibitor
- Agonist at cholinergic N2 receptors (inhib Achase) at peripheral sites (results in increased Ach at N2 receptors of NMJ and muscarinics-heart, salivary)
-
Neostigmine Uses
- postoperative paralytic ileus
- atony of GI/GU
- MG
- reversal of mm paralysis from competitive nm blocking stuff like D-tubocurarine
-
Pyridostigmine
- mestinon
- carbamate Achase inhibitorAgonist at cholinergic N2 receptors (inhib Achase) at peripheral sites (results in increased Ach at N2 receptors of NMJ and muscarinics-heart, salivary)
-
-
Carbaryl MOA
- sevin
- irreversible organophosphate inhibitor of Ach (carbamate Achase inhibitor)
-
Dimpylate MOA
- diazinon
- organophosphate Achase inhibitors
- Active site of Achase is phosphorylated and rate of hydrolysis of enzyme is not really slow
-
Parathion MOA
organophosphate Achase inhibitor (phosphorylates AS to make enzyme slow)
-
Parathion pharm effects
converted to active metabolite paraoxon by CYP450
-
Malathion MOA
- organophosphate Achase inhibitor
- As of Achase is phosphorylated and rate of hydrolysis of enzyme is now really slow
-
-
Malathion AE
- Serious: burns
- Common: skin irritations
-
Pralaxidome MOA
- protopam
- accelerates hydrolysis of phosphate enzyme at NMJ (does not enter CNS)
-
Pralidoxime uses
antidote to insectide poisoning
-
Atropine MOA
muscarinic antagonist; tertiary
-
Scopolamine MOA
muscarinic receptor antagonist
-
Scopolamine pharm effects
- reverses block from D-tubocurarine
- tranquilizer
-
Scopolamine uses
surgery, motion sickness, parkinsonism, spastic muscle states, irritable bowel syndrome, diverticulitis
rx anteiror uveitis, keratitis, choroiditis (relaxes sphincter and ciliary mm to decrease pain)
-
Cyclopentolate MOA
muscarinic receptor antagonist; tertiary
-
Cyclopentolate uses
DOC for mydriasis in eye exam bc short duration
-
Atropine uses
rx anteiror uveitis, keratitis, choroiditis (relaxes sphincter and ciliary mm to decrease pain)
-
Tropicamide MOA
muscarinic receptor antagonist; tertiary
inhibits response of sphincter and ciliary eye mm
-
Tropicamide uses
used in fundoscopic exam for mydriasis because shortest duration
-
Benztropine MOA
muscarinic receptor antagonist; tertiary
-
Trihexyphenidyl MOA
muscarinic receptor antagonist; tertiary
-
Trihexyphenidyl
treats mm stiffness as in Parkinson's
-
Dicyclomine MOA
- muscarinic receptor antagonist; tertiary
- bentyl
-
Dicyclomine Uses
- relieves GI muscle spasms
- rx IBS
-
Hyoscyamine MOA
- muscarininc receptor antagonist; tertiary
- levsin
-
Hyoscyamine Uses
- relief from muscle spasms
- reduces the fluid secretions of many organs and glands
- including peptic ulcers, IBS
- control mm spasms in the bladder, kidneys, GI, and to reduce stomach acid.
- reduce tremors and rigid mm in Parkinson's
- drying agent to control excessive salivation, runny nose, or excessive sweating
-
Oxybutynin MOA
- muscarinic receptor antagonist; tertiary
- Ditropan XL
-
Oxybutynin pharm effect
blocks muscarinic receptors and gives antispasmodic effect on detrusor mm so that spontaneous contractions in the bladder are decreased and allows increased bladder storage and decreased frequency
-
Oxybutynin Uses
overactive bladder
-
Tolterodine MOA
- muscarininc receptor antagonist; tertiary
- detrol
-
Tolterodine AE
somnolence, dry mouth, blurred vision, constipation
-
Tolterodine usese
overactive bladder
-
Solifenacin MOA
muscarinic receptor antagonist; tertiary
-
Solifenacin uses
overactive bladder
-
Darifenacin MOA
- selective muscarinic receptor antagonists; tertiary
- enablex
-
Darifenacin AE
less dry mouth, nothing else really
-
Diphenydramine MOA
muscarinic receptor antagonists; tertiary
-
Diphenydramine Uses
aka benedryl
-
N-methylatropine
muscarinic receptor antagonist; quaternary
-
Methscopolamine MOA
muscarinic receptor antagonist; quaternary
-
Methscopolamine AE
impair your vision, thinking, or reactions
-
methscopolamine uses
reduce stomach acid secretions and rx peptic ulcers
-
Tiotropium MOA
muscarinic receptor antagonist; quaternary
-
Tiotropium uses
prevent bronchospasm in people with bronchitis, emphysema, or COPD
-
Tiotropium pharm effects
bronchodilation
-
Ipratropium MOA
muscarinic receptor antagonist; quaternary
-
Ipratropium uses
prevent bronchospasm in people with bronchitis, emphysema, or COPD
-
Ipratropium pharm effects
bronchodilation
-
Glycopyrrolate MOA
muscarinic receptor antagonist; quaternary
-
Glycopyrrolate uses
peptic ulcers and reduce drooling in kids
-
Nicotine MOA
- nicotinic receptor agonists; direct stimulation of peripheral N1/N2 cholinergics
- In the CNS: stimulates N1 cholinergics to release NE and DA and increase/decrease Ach release
-
Nicotine pharm effects
acute CNS and cardio stuff (see notes)
-
Trimethaphan MOA
N1 receptor antagonist/ ganglionic blocking
-
Epinepherine
adrenergic agonist
-
Dopamine
adrenergic agonist
-
dobutamine
- adrenergic agonist; stimulates B1>B2
- racemic mixture of entantiomers
-
dobutamine uses
short term rx for cardic decompensation
-
-
Dobutamine pharm effects
- Positive ionotropic: B1 receptor stimulation will increase SV
- Arteriolar VD: B2 receptor stimulation lowers TPR so that DBP falls
- Venodilation: B2 receptor stimulation will decrease VR and decrease cardiac filling P in pts w/ MI
-
Isoproterenol pharm effects
- + ionotropic and chronotropic effects in cardiac arrest
- increase in AV conduction in AV block
-
Salmeterol MOA
- adrenergic agonist
- serevent
- B2>>B1
-
Salmeterol Pharm effects
relieves bronchoconstriction of asthma, COPD, bronchitis
-
Salmeterol uses
asthma, COPD, bronchitis
-
Terbutaline MOA
- adrenergic agonist
- bricanyl, brethine
- B2>>B1
-
Terbutaline uses
bronchospasms, asthma, bronchitis
-
terbutaline pharm effects
bronchodilator: relaxes mm in airway
-
Albuterol MOA
- adrenergic agonist
- Ventolin, provetil
- B2>>B1
-
Albuterol uses
bronchospasms
-
Albuterol pharm effects
bronchodilator to relax mm in airway to lungs
-
Ritodrine MOA
- adrenergic agonist
- Yutopar
- B2>>>>B1
-
Ritodrine uses
- delays birth
- used to achieve external version of fetus from breach to vertex before birth
-
Ritodrine pharm effects
relaxes uterine sm mm
-
Phenylephrine MOA
- adrenergic agonist
- A1 only
- neo-synephrine
-
Phenylephrine pharm effects
- systemic VC
- constricts blood vessels in nasal mucosa (relieves congestion)
- contracts radial mm (mydriasis)
-
Ritodrine uses
- fundoscopic exams (mydriasis via contracting radial mm)
- relieves nasal congestion (constricts blood in nasal mucosa)
-
Oxymetazoline MOA
- adrenergic agonist
- Afrin
- A only
-
Oxymetazoline uses
nasal decongestant (better than phenylephrine)
-
Tyramine MOA
- adrenergic agonist
- indirectly acting
-
Tyramine pharm effects
releases endogenous NE that has been stored until now; increases BP since releasing NE from sympathetic nerves that innervated blood vessels
-
Tyramine uses
in fermented food; must be taken IV because will be destroyed in gut if taken p.o.; cannot cross BBB so effects are confined to periphery
-
Amphetamine MOA
- adrenergic agonist
- lipid soluble so can enter CNS and release NE from central AND peripheral adrenergic neurons; blocks neuronal uptake of NE and will cause release of DA in NA
-
Amphetamine pharm effects
lipid soluble so can enter CNS and release NE from central AND peripheral adrenergic neurons; blocks neuronal uptake of NE and will cause release of DA in NA
-
Ephedrine MOA
- adrenergic agonist; mixed
- lipid soluble-->enters CNS to act at B1 and B2 directly
-
Ephedrine pharm effects
- Acts directly at both B1 and B2 via NE
- Direct B: bronchodilation in asthma and increases AV conduction
- Indirect A: mydriasis, increases BP, nasal decongestion
-
Ephedrine uses
asthma, mydriasis, nasal decongestant, reverses hypotension in anesthesia
-
Pseudoephedrine MOA
- adrenergic agonist
- mixed, lipid soluble; goes into CNS
- sudafed
-
Pseudoephedrine uses
nasal and sinus decongestant
-
Pseudoephedrine AE
insomnia
-
Pseudoephedrine pharm effects
since it is a stereoisomer of ephedrine; there is less CNS excitation and less BP/HR increases
-
Phenoxybenzamine MOA
- alpha adenoceptor antagonist
- dibenzyline
- non competitive receptor block results from covalent binding of receptor
- A1>>A2
-
Phenoxybenzamine uses
reduce BP and sweating (pheochromocytoma ppl sweat a lot)
-
Phentolamine MOA
- A adrenoceptor antagonist
- regitine
- A1 = A2
-
Phentolamine uses
dental anesthesia reversal
-
Prazosin, terazosin, doxazosin MOA
- A adrenoceptor antagonist
- minipress, hytrin, cardura respectively
-
Tamsulosin MOA
- A adrenoceptor antagonist
- flomax
- A1 only
-
tamsulosin pharm effects
Tamsulosin relaxes the muscles in the prostate and bladder neck, making it easier to urinate.
-
Tamsulosin uses
improve urination in benign prostatic hyperplasia
-
Labetalol MOA
- A adrenoceptor antagonist
- trandate, normodyne
- Blocks B1 and A1
-
Labetalol uses
hypertension treatment
-
Yohimbine MOA
- A adrenoceptor antagonist
- A1<<<A2
- yohimex, yocon
-
Yohimbine pharm effects
- CNS
- Central A2 block in baroreflex arc will increase preganglionic sympathetic nerve activity to cause tachycardia, tremor, increase in BP
-
Yohimbine AE
restlessness, irritability, anxiety, no boners
-
Ergotamine, dihydroergotamine MOA
-
A adrenoceptor antagonist (partial agonist)
ergostat/cafergot
-
Ergotamine and Dihydroergotamine pharm effects
- constrict cerebral blood because partial A agonist
- stimulates alpha adrenergic receptors, producing peripheral vasoconstriction and decreased blood flow; exhibits serotonin antagonistic properties
-
Ergotamine and dihydroergotamine uses
treat migraine like headaches (remember it constricts blood flow in brain!)
-
Phentolamine MOA
A adrenoceptor antagonist
-
Phentolamine pharm effects
reverses ischemia and tissue necrosis via extravation of DA from veins
-
Phentolamine uses
treats impotence
-
Alprostadil MOA
relaxes arterial smooth muscle, producing vasodilation; inhibits platelet aggregation (prostaglandin E1)
-
Alprostadil uses
treats impotence/ED (can be a topical use)
-
Betaxolol
- B adrenoceptor antagonist
- Kerlone
- cardio selective
-
Betaxolol uses
treats hypertension
-
Atenolol MOA
- B adrenoceptor antagonist
- cardio selective
-
Atenolol uses
treat hypertension, treat/prevent heart attacks, treat angina
-
Metoprolol MOA
- B adrenoceptor antagonist
- lopressor, toprol
- cardio selective
-
Metoprolol uses
angina, hypertension, heart attack
-
Esmolol MOA
- B adrenoceptor antagonist
- breviblock
- cardio selective
-
Esmolol uses
rapid control of ventricular rate
-
Propranolol MOA
- B adrenoceptor antagonist
- not selective
- Inderal
-
Propranolol uses
tremors, angina, hypertension, heart rhythm disorders, treat or prevent heart attack, and to reduce the severity and frequency of migraine headaches
-
Timolol MOA
- B adrenergic antagonist
- biocadren
- non selective
-
Timolol uses
hypertension
-
Labetalol MOA
- B adrenoceptor antagonist
- trandate
- non selective
-
Labetalol uses
hypertension
-
Alpha methyldopa MOA
- sympathoyltic
- Aldomet
- Transported into central/peripheral noradrenergic via aromatic AA pump and is converted to alpha-methylNE; this will NOT be metab by MAO and will be stored in cytoplasm AND vesicles as a result
- Also stored as nt in noradrenergic neurons and will be released by AP
- See notes
-
Alpha methyldopa pharm effects
- VC (just as well as NE)
- Blood: net balanced vasodilation
- Heart: HR decreases, myocardial oxygen demand decreases
- Pituitary: PL secretion increases
-
Alpha methyldopa uses
hypertension in kids and pregnant women
-
Reserpine MOA
- sympatholytic; alkaloid from plants
- Seprasil
- Destroys IC vesicles for nt in peripheral/central monoaminergics which results in depleted net stores
-
Reserpine pharm effects
- Small doses: deplete peripheral sympathetic monoaminergic stores only
- Blood: decreases amount of NE released, net balanced VD
- Heart: HR and CO little change
- GI: increased motility and tone from unopposed PS
- Pituitary: PL secretion increases because DA depleted
-
reserpine uses
hypertension, psychotic states?
-
Guanethidine MOA
- sympatholytic; adrenergic neuronal blocker
- poor lipid solubility
- directly inhibits NE release from peripheral sympathetic neurons
- Ismelin
-
-
Guanethedine pharm effects
- Blood: net balanced VD
- Heart: HR and CO unchanged
-
Guanethidine AE
orthostatic hypotension, sex dysfx, supersensitive to direct sympathomimetic amines (adrenoceptors are upregulated), unopposed PS activity
-
Cocaine MOA
- alkaloid
- neuronal NE uptake 1 transporter
- Local anesthesia via blocking Na channels in pain fibers-->non comp block monoamine uptake 1 in c/p neurons-->amp postj/s NE, DA, Epi, Serotonin effects
- Increases peripheral sympathetic outflow
- Increased DA stimulation in NA (euphoria)
-
Cocaine Pharm effects
- (See notes)
- local anesthesia, CNS, dose related, indirect VC, local hemostasis
-
-
Cocaine uses
anesthesia in eye and nose surgery
-
Reserpine AE
- (see notes)
- Teratogenic
- CNS
- orthostatic hypertension
- sex dysfx
- hyperprolactinemia
- supersensitive to direct sympathomimetic amines
- unopposed PS activity
-
Alpha methyldopa AE
sedation, dry mouth, congestion, edema, orthostatic intolerance, flu sx, + Coombs, HS rxn for hepatitis, hyperprolactinemia
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