PLE: PHARMA PEARLS Flashcards
Master Pharma with the help of Topnotch Medical Board Prep PEARLS
CYTOCHROME P450 INDUCERS MNEMONIC
Ethel Booba takes Phen-Phen and Refuses Greasy Carb Shakes
Cytochrome P450 Inducers
Ethanol (chronic ingestion) Barbiturates exceot SECOBARBITAL Phenytoin Rifampicin Griseofulvin Carbamazepine St. John's Wort/Smoking *Glutethimide, Phenylbutazone, chronic/repeated use of Ritonavir
CYTOCHROME P450 INHIBITORS MNEMONICS
Inhibitors Stop Cyberkids From Eating Grapefruit QV
CYTOCHROME P450 INHIBITORS
Isoniazid Sulfonamides Cimetidine Ketoconazole Erythromycin Grapefruit Juice Ritonavir (acute ingestion) Amiodarone Quinidine Valproic Acid
OTHER CYP450 INHIBITORS (12)
Allopurinol, Chloramphenicol, Chlorpromazine, Dicumarol, Disulfiram, Ethanol (acute toxicty), Itraconazole, Nortriptyline, OCP, Phenylbutazone, Saquinavir, Secobarbital, Spironolactone, Troleandromycin
Drugs with NARROW THERAPEUTIC INDEX mnemonics
WALA na Cyang Papa! VasTeD na!
Drugs with NARROW THERAPEUTIC INDEX (10)
Warfarin Aminoglycosides Lithium Amphotericin B Carbamzepine Phenobarbital Phenytoin Vancomycin Theophylline Digoxin
Drugs that display ZERO ORDER KINETICS mnemonics
WHAT PET
Drugs that display ZERO ORDER KINETICS (7)
Warfarin Heparin Aspirin Tolbutamide Phenytoin Ethanol Theophylline
Drugs that display TACHYPHYLAXIS mnemonics
MEDical students Love to watch CNN in HD!
Drugs that display TACHYPHYLAXIS (9)
Metoclopramide Ephedrine Dobutamin LSD Calcitonin Nitroglycerin Nicotine Hydralazine Desmopressin
PHASE 1 of drug study
Is the drug safe?
Dose-response relationship, normal human volunteers, acute effects
PHASE 2 of drug study
Is the drug effective for the sick patient?
Placebo, usually in the hospital, sick patients
PHASE 3 of drug study
Randomized, double-blind, controlled trials
Special population, very expensive
PHASE 4 of drug study
Post-marketing surveillance
Infrequent toxicities
Pregnancy Category A
Safe in controlled studies of women
Fetal harm is remote
Pregnancy Category B
No controlled studies in women
No risk in animal reproduction studies
OR
Not confirmed in controlled studies in women
No AE in animal reproduction studies
Pregnancy Category C
No controlled studies in women
With AE in both animal studies
OR
Give only if benefit > risk
Pregnancy Category D
(+) AE but Benefits > Risk
Pregnancy Category X
(+) AE, Contraindicated
Alpha 1 location and action
Alpha 1 in smooth muscles for vasconstriction
Alpha 2 location and action
Alpha 2 in nerve terminals for inhibition of NT release
Alpha 1 preferred substrate
Epinephrine
Alpha 2 preferred substrate
Epinephrine
Beta 1 location and action
Beta 1 in heart to increase rate and contractility
Beta 1 preferred substrate
Isoproterenol > Epinephrine > Norepinephrine
Beta 2 location and action
Beta 2 in respiratory smooth muscles and uterus for bronchodilation and uterine relaxation
Dopamine 1 location and action
Dopamine 2 in splanchnic and renal vessels for vasodilation of renal blood vessels
Dopamine 2 location and action
Dopamine 2 in nerve terminals of CNS for regulation of NT
Muscarinic 1 location and action
Muscarinic 1 in CNS for stimulation
Muscarinic 1 preferred substrate
Acetylcholine
Muscarinic 2 location and action
Muscarinic 2 in heart for decreasing heart rate
Muscarinic 2 preferred substrate
Acetylcholine
Muscarinic 3 location and action
Muscarinic 3 in smooth muscle, GIT, GUT, pulmonary, and eyes for peristalsis, bladder contraction, bronchoconstriction, and pupil constriction
Muscarinic 3 preferred substrate
Isoproterenol > Epinephrine > Norepinephrine
Ach cholinergic inhibitor of its SYNTHESIS
Hemicholinium
Ach adrenergic inhibitor of its SYNTHESIS
Metyrosine
Ach cholinergic inhibitor of its STORAGE
Vesamicol
Ach adrenergic inhibitor of its STORAGE
Reserpine
Cholinergic inhibitor of Ach RELEASE
Botulinum
Adrenergic inhibitor of Ach RELEASE
Guanethidine
Cholinergic inhibitor of ACh metabolism
Neostigmine
Adrenergic inhibitor of Ach metabolism
MAOIs, COMTs
Cholinergic inhibitor of Ach REUPTAKE
NONE
Adrenergic inhibitor of Ach REUPTAKE
Cocaine, TCAs
How does EDROPHONIUM differentiate MYASTHENIC crisis from CHOLINERGIC crisis?
Edrophonium IMPROVES muscle strength in MYASTHENIC crisis and WEAKENS muscle strength in CHOLINERGIC crisis.
Spinal roots of origin of SNS
T1-T12 and L1-L5
Location of ganglia of SNS
Paravertebral chains that lie along the spinal columnm some along the anterior aspect of the abdominal aorta
Distance of preganglionic fibers of SNS
Short
Distance of postganglionic fibers of PNS
Long
Spinal roots of origin of PNS
CN III, VII, IX, X
Sacral segments of spinal cord
Location of ganglia of PNS
Most are in organs innervated more distant from the spinal cord
Distance of preganglionic fibers of PNS
Long
Distance of postganglionic fibers of PNS
Short
Direct acting muscarinic 3 receptor for bladder and bowel atony
Betanechol
M3 cholinomimetic for glaucoma and Sjogren and Sicca syndrome
Pilocarpine
Selective M3: Cevimeline
Indirect acting cholinomimetic for diagnosis of Myasthenia Gravis
Edrophonium (Tensilon Test)
ACE inhibitors teratogenic effect
fetal renal damage
Antiepileptic drugs teratogenic effect
neural tube defect
Phenytoin teratogenic effect
fetal hydantoin syndrome
Barbiturates teratogenic effect
neonatal dependence
Diethylstilbestrol (DES) teratogenic effect
Vaginal clear cell adenoCA
Ethanol teratogenic effect
fetal alcohol syndrome
LIthium teratogenic effect
Ebstein’s anomaly
(septal and posterior leaflets of the tricuspid valve are displaced towards the apex of the right ventricle of the heart)
Isoretinoin teratogenic effect
craniofacial malformations
Iodide teratogenic effect
congenital hypothyroidism
Misoprostol teratogenic effect
Mobius sequence
Palsy of CNs, usually VI and VII
Penicillamine teratogenic effect
cutis laxa
(chalazoderma, dermatochalasia, dermatolysis, dermatomegaly, generalized elastolysis, generalized elastorrhexis, or pachydermatocele)
the skin becomes inelastic and hangs loosely in folds
Thalidomide teratogenic effect
phocomelia
Smoking teratogenic effect
IUGR
Tetracycline teratogenic effect
tooth discoloration
Streptomycin teratogenic effect
ototoxicity
Methimazole teratogenic effect
aplasia cutis congenita
Sulfonamide teratogenic effect
kernicterus
Fluoroquinolone teratogenic effect
cartilage damage
Warfarin teratogenic effect 1st trimester
chondrodysplasia
Warfarin teratogenic effect 2nd trimester
CNS malformation
Warfarin teratogenic effect 3rd trimester
bleeding diatheses
SNS effect on pupils (general)
mydriasis (alpha 1)
miosis (M3)
SNS on iris
Contraction of dilator pupillae muscles (radial muscles)
mydriasis(α1)
PNS on iris
Contraction of sphincter pupillae muscles (circular muscles)
miosis (M3)
SNS on ciliary muscle
Relaxation for distant vision (β2)
PNS on ciliary muscle
Contraction (M) for accommodation of lens (near vision) and increase aqueous humor outflow into canal of Schlemm
SNS on ciliary body epithelium
Increased aqueous humor production (β1)
PNS on ciliary body epithelium
None
SNS on heart contractility
Increased via B1
PNS on heart contractility
Decreased via M2
SNS on skin and splanchnic blood vessels
Constriction via A1
PNS on skin and splanchnic blood vessels
NO EFFECT
SNS on skeletal blood vessels
Dilation via B2 and M3
PNS on skeletal blood vessels
NO EFFECT
SNS on bronchi
Dilation via B2
PNS on bronchi
Constriction via M3
SNS on GIT walls
Relaxation via A2 and B2
PNS on GIT walls
Contraction via M3
SNS on GIT secretion
NO EFFECT
PNS on GIT secretion
Increased via M1 and M3
SNS on bladder wall
Relaxation via B2
PNS on bladder wall
Contraction via M3
SNS on uterus
Contraction via A1
Relaxation via B2
PNS on uterus
Contraction via M3
SNS on penis
Ejaculation via alpha
PNS on penis
Erection via muscarinic
SNS on sweat glands
Increased sweating via alpha
PNS on sweat glands
NO EFFECT
SNS on liver
Gluconeogenesis, glycogenolysis (Alpha, B2)
PNS on liver
NO EFFECT
SNS on fat cells
Lipolysis (B3)
PNS on fat cells
NO EFFECT
SNS on kidney
Increased renin secretion via B1
PNS on kidney
NO EFFECT
Effect of Gq protein stimulation on M1, M3, and M5 receptors
↑ IP 3 , DAG cascade
Effect of Gi protein stimulation on M2 and M4receptors
↓ cAMP synthesis
Effect of stimulation of Nn/Ng (ganglion) and Nm (neuromuscular) receptors
Na + /K + depolarizing current
ORGANOPHOSPHATE POISONING
DUMBBELSS
DUMBBELSS
ORGANOPHOSPHATE poisoning
Diarrhea, urination, miosis, bronchoconstriction, bradycardia, excitation of SkM & CNS, lacrimation, salivation, sweating
ATROPINE TOXICITY
Hot as a hare Dry as a bone Red as a beet Blind as a bat Mad as a hatter
Inhibits synthesis of catecholamines via inhibiting hydroxylation of tyrosine to dopamine
Metyrosine
Inhibits synthesis of acetylcholine by blocking choline transport
Hemicholinium
Inhibits storage of Ach into vesicles via VAT
Vesamicol
Alters synaptobrevin to prevent release of Ach
Botulinum toxin
Inhibits acetylcholinesterase
Carbamates and organophosphates (indirect acting cholinomimetics)
Increase stores of NE and dopamine by blocking its metabolism
MAOIs
Inhibits release of catecholamines via VAMPs and SNAPs
Guanethidine
Promotes increased release of catecholamines
Ampheramines and tyramines
Inhibits diffusion and reuptake of catecholamines via NET and DAT
cocaine, tricyclic antidepressants
Inhibits reuptake of acetylcholine
NONE
Low dose dopamine (1-5 mcg/kg/min) acts on
D1 receptors (to increase RBF and UO)
Medium dose dopamine (5-15 mcg/kg/min) acts on
B1 receptors
High dose dopamine (>15 mcg/kg/min) acts on
alpha receptors (increase CO and BP)
Non-selective beta agonist that can be used for asthma or AV block
isoprotenerol
Antidote for alpha 1 agonist overdose
phentolamine
Phenylephrine, pseudoepehdrine, oxymetazoline all act on what receptor to produce nasal decongestion
Alpha 1
Side effectof phenylephrine, pseudopehedrine, oxymetazoline
Rebound nasal congestion (rhinitis medicamentosa)
MOA of clonidine
When given orally, they accumulate in the CNS to decrease central sympathetic outflow
Pregnancy category of methyldopa
B
Alpha 2 agonist that decreases CNS sympathetic outflow for pre-eclampsia and gestational HPN
methyldopa
Alpha 2 agonist used for reducing conscious sedation
dexmedetomidine
Alpha 2 agonist used as muscle relaxant
tinazinidine
Side effect of methyldopa
(+) Coomb’s test - hemolytic anemia
Alpha 2 agonist used in glaucoma to decrease secretion of aqueous humor
apraclonidine, brimonidine
Side effect of dobutamine
tachyphylaxis
General clinical use of alpha 1 agonist
Hemostasis (epinephrine locally)
Decongestion
Spinal shock
General clinical use of alpha 2 agonist
Hypertension
Glaucoma
General clinical use of beta 1 and dopa 1 agonsit
Acute heart failure
Septic shock
General clincal use of beta 2 agonist
Bronchospasm
Premarture labor
Has a direct adrenergic receptor agonist aside from causing release of NE;
Nasal vasoconstrictor and appetite stimulant
phenylpropanolamine
Adverse effect of phenylpropanolamine
hemorrhagic stroke
Longest acting Beta blocker
Nadolol
non-selective beta blocker that can cause reduction in size of infantile hemangioma
propanolol
beta blockers for heart failure
labetolol, carvedilol, metoprolol
Irreversible non-selective alpha blocker used for pre-op of pheochromocytoma
phenoxybenzamine
Reversible non-selective short acting alpha antagonist for rebound hypertension
phentolamine (tolazoline)
Disadvantage of using betablockers in the eye
Local anesthetic activity (membrane stabilizing activity)
Decreased protective reflexes
Beta blockers with partial agonist activity
(with intrinsic sympathomimetic activity)
beneficial for asthma bec less bronchospasm
Acebutolol Pindolol Carteolol, Celiprolol Bopindolol Penbutolol
Beta 1 blocker used parenterally for SVT
esmolol
Teratogenic effect of atenolol
Low BW and impaired fetal growth
Beta blocker for decreasing secretion of aqueous humor
timolol
Osmotic agent for decreasing aqueous humor
mannitol
Alpha 2 agonist for decreasing aqueous humor
apraclonidine
Carbonic anhydrase inhibitor for decreasing aqueous humor
acetazolamide
dorzolamide
Cholinomimetics for ciliary muscle contraction causing opening of trabecular meshwork, and increased aqueous humor outflow
pilocarpine
physostigmine
Prostaglandin that increases outflow through canal of Schlemm
latanoprost
Non-selective alpha agonist that increases outflow via uveoscleral veins
epinephrine
Beta blockers with combined alpha and beta blocking actions
Do not cause epinephrine reversal
Labetalol
Carvedilol
Chronic use of beta blockers contributes which mechanism for anti hypertension?
Chronic use of beta blockers can cause decreasenin vascular resistance from reduced renin release from kidney
A newer beta blocker that has some direct vasodilator action caused by NO release
Nebivolol
Anti hypertensive (sympathoplegic directly acting on CNS) that is associated with positive Coombs test
Methyldopa
Calcium channel blocker associated with lupus like syndrome
Hydralazine
Common electrolyte imbalance caused by aliskiren and other RAAS blockers
Hyperkalemia