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147 Cards in this Set

  • Front
  • Back
Pharmacodynamics
Is the study of impact of drugs on the body, it includes organ effects, mechanism and adverse effects of drugs
Pharmacokinetics
Is a branch dedicated to the determination of the fate of drugs administered externally to a living organism. It deals with ADME
Absoption
drug to systemic circulation
distribution
drug from systemic circulation to organ
Elimination
Through liver and kidney
Metabolism
From systemic circulation to liver or kidney
NSAIDs
inhibit cycloxygenase 1 and 2, leading to reduction of PGs formation
Function of ABC exporters (ATP binding cassette)
expels foreign molecules
Phase I rxns
introducing or unmasking a function group to the structure of parent drugs (oxidation, reduction, deamination and hydrolysis)
Phase II rxns
conjugation of subgroups to a functional group
P450
18 families
43 subfamilies
57 genes
Phase II products are water soluble or insoluble
water soluble
Potency refers to
the amount of drug needed to produce an effect. dose to produce 50% of the maximal effect EC50
Efficacy
Is defined as potential maximum therapeutic response Emax that a drug causes.
Emax
the maximal therapeutic effect caused by a drug
TD50
Median toxic dose
LD50
median lethal dose
TI = TD50/ED50
Therapeutic Index
5 receptors
1. Intracelullar(steroid, thyroid)
2. membrane receptors that have enzyme activity(insulin)
3. membrane receptors that bind to tyrosine kinase molecules (cytokines)
4. Membrane receptors that have ion channel function(ACh, GABA, serotonin)
5. Membrane receptor that are coupled with G proteins (DA, NE, 5-HT)
Down regulation of receptors
Caused by agonists
Up regulation of receptors caused by
antagonists
Phase I
Is it safe? uses volunteers
Phase II
Dose it work in patients
Phase III
does it work by double blind
Phase 4
postmarketing surveillance
IND
investigational New Drug
Criterion as NT
1. precursor within the presunaptic membrane
2. chemical can be triggered and released by action potentials
3. receptors are located in postsynaptic and presynaptic by action potentials
4. a biochemical inactivation is observed
M1
CNS and glands
contraction of myenteric plexus
M2
Heart, CNS
Decreased heart activity
M3
SM, lungs and glands
Bronchial contraction
M4
CNS
M5
Gq protein
B1
Heart contractility, stimulates kidney release of renin
B2
relaxes SM, but skeletal muscle vessel dilation
B3
increases lipolysis
A1
SM contraction, glands, stimulates sphincters, increased BP
A2
relaxes SM in GI
inhibits secretions, decreased intraocular pressure by blockage of formation of aquous humor
Isoproterenol and Dobutamine
B1 agonists
Propranolol, Nadolol, Timolol
nonselective B blockers
Combined alpha and beta blockers
Carvedilol and Labetanol
B2 blocker
Butoxamine
B2 agonists
Albuterol, Epinephrine, NE and Terbutaline
albuterol, epinephrine, NE and terbutaline
B2 agonists
B1 blockers
Acebutolol, atenolol, esmolol, metoprolol
Nn
ANS ganglia
Nm
Neuromuscular endplate depolarization
Muscrine, Pilocarpine and bethanechol
Muscurinic agonist
Atropine
M antagonist
M1 blockers
pirenzepine, Dicyclomine
M2 blocker
AF-DX116
N agonists
Nicotine, varenicline, lobeline
Nn blocker
tubocurarine, succinylcholine
ChE inhibitors
Neostigmine, physostigmine, parathion, edrophonium
ChE regenerator compound
Oxime agents PAM and atropine
A1 agonist
Phenylephrine
A1 blocker
Prazosin, terazosin, doxazosin, tamsulosin,
nonselective A blockers
phentolamine
Clonidine
A2 agonist
A2 antagonist
yohimbine
Thiopental has hypoalgesia or hyperalgesia?
hyperalgesia
Ketamine blocks what channel?
glutamate
What drug has the emergence phenomenon?
Ketamine
Local anesthetics block what channel?
Na+ channel
Cocaine blocks?
NE reuptake
What is the most widely used local anesthetic?
Lidocaine
AE's of local anesthetics
CNS excitation, convulsion, especially with esters
DOA can be increased by adding a vasoconstrictor or any adrenergic agonist like NE with what type of drugs?
local anesthetics
Parkinson's Disease
damage to DA neurons
Mesolimbic pathway
reward and addictive pathway
Nigrostriatal controls
voluntary movement
Strategies to treat PD
replace DA
Give DA agonist or block DA catabolism
DA act at the what receptors?
D2
Pramipexole, Ropinerole, Bromocriptine, pergolid, selegiline
used for PD
COMT inhibitors
Tocapone and entacapone for PD
Huntington's Chorea
GABAnergic neurons degenerate
Treatment of HC
fluoxetine, carbamazepine, tetrabenzepine
Alzheimer's Disease
marked atrophy of cerebral cortex, severe degeneration of cholinergic neurons
AD treatment with cholinesterase inhibitors
Tacrine, Donepezil, rivastigmine, galantamine, memantidine
Positive symptoms of Schizophrenia
hallucination, delusion, disorganized and illogical thought
Negative symptoms
flat emotional expressiveness, social isolation or withdrawal
Is pathogenesis known of schizophrenia?
no
Older/typical antipsychotics treat positive or negative symptoms?
Positive
Atypical antipsychotics block 5-HT2A or D2 more?
5-HT2A more
which atypical antipsychotic can cause agranulocytosis?
Clozapine
What are the hypothesis associated with depression?
Monoamine and neurotropic
General mechanisms to treat depression are increase synaptic availabiity of:
NE and serotonin
SSRI's
fluoxetine, sertraline, paroxetine
SNRI's
venlafaxine, duloxetine and TCA's
5-HT2 antagonists
Trazadone
What are the hypothesis associated with depression?
Monoamine and neurotropic
General mechanisms to treat depression are increase synaptic availabiity of:
NE and serotonin
SSRI's
fluoxetine, sertraline, paroxetine
SNRI's
venlafaxine, duloxetine and TCA's
5-HT2 antagonists
Trazadone
Tetracyclic and unicyclic antidepressants
amoxapine, bupropion
MAOI's
Phenezine, tranylcypromine
Mood stabalizing agents
lithium, carbamazepine, valproic acid
Constipation is a common side effect with what type of drug?
opiods
Naloxone
opioid antagonist
Naltrexone, nalmefene
opioid antagonists
fentanyl is how many times more potent than morphine?
100
What is tetrahydrocannavinoid?
PHC
What is the gateway drug?
Cannavinoids
Amphotericin B MOA
binds to ergosterol in the fungal cell membrane, forms channels and increases membrane permeability
Amphotericin B AEs
infusion rxns
nephrotoxicity
hypokalemia and hypomagnesemia
anemia
Azole antifungal MOA
inhibit 14-a-sterol demethylase
what would you use for aspergillus or candida infection?
caspofungin only used IV
caspofungin MOA
inhibits synthesis of funga cell wall by inhibiting synthesis of B-(1,3)-D-glucan
Is Flucytosine a prodrug?
Yes, MOA is 5-FUMP
Flucytosine AEs
bone marrow suppression
rash
N,V,D
elevated LFTs
Griseofulvin static or cidal?
static, inhibits fungal cell mitosis
Griseofulvin is used for?
dermatophytic infection
which drug is similar to Amphotericin B?
Tolnaftate
which drug is uses for oral candidiasis?
Tolnaftate
What drug causes redness, alopecia, hair discoloration and nail disorders with the lacquer?
Ciclopirox
Do Allylamines cause neutropenia?
Yes
Isoniazid is cornerstone of treatment for?
TB
AEs of Isoniazid?
Peripheral nuropathy
hepatotoxicity
immunologic mediated fever and skin rashes
systemic lupus erythematosus-like syndrome
Streptomycin is an aminoglycoside, can it be given orally?
No
Rifabutin is good for HIV patients bc:
Less p450 enzyme induction
What antibiotics can't be used in infants?
Chloramphenicol
(gray baby syndome)
Sulfonamides
(kernictirus,bilirubin)
What antibiotics can't be used in children?
Tetracyclines
(teeth discoloration)
fuoroquinolones
(tendonitis)
What antimicrobials can you not drink alcohol with?
cephalosporins and metrinodazole
Cell wall active
bactericidal
penicillins cidal or static?
Cidal
Cephalosporins cidal or static?
cidal
Do penicillins have trouble with gram - bacteria?
Yes bc small peptidoglycan layer
what generation of cephalosporins cross the BBB?
3rd and 4th
carbapenems cidal or static?
cidal
what type of administration are carbapenems given?
only parental administration
monobactams cidal or static?
cidal
vanco broad or narrow?
Narrow (gram +)
what antibiotic has red man syndrom and ototoxicity?
vanco
Tetracyclines cidal or static?
static
Uses of tetracyclines?
atypical and community acquired pneumonia, chamydia, tularemia from rabbit, rocky mountain spot fever, acne, lyme's PUD and anthrax
Macrolides cidal or static?
static
macrolides broad or narrow?
broad and atypical coverage
what is used for treating MAC?
clarithromycin
Ketolides broad or narrow?
narrow
What is special about quiupristin/Dalfopristin?
make sure to infuse IV oer at least one hour with D5W and not saline
Aminoglycosides cidal or static?
cidal
aminoglycosides AEs
otoxicity and neuromuscular blockade
Quinolones cidal or static?
cidal
Sulfonamides cidal or static?
static
Polymixin B cidal or static?
cidal
Sulfonamides cidal or static?
static
Polymixin B cidal or static?
cidal