Block 3 Review Flashcards
mechanism of action of amphotericin B
creates pores in cell membrane
how is toxicity of amphotericin B reduced
liposomal preparation
slow infusion rate
adverse effect of amphotericin B
nephrotoxicity
what antifungal crosses BBB and achieves good CSF
flucytosine
flucytosine mechanism of action
inhibition of thymidylate synthetase
azole mechanism of action
inhibition of 14alpha demethylase
ketoconazole mechanism of action
inhibition of microsomal enzymes
adverse effects of ketoconazole
endocrine effects (blocks androgen receptors)
disulfiram-like reaction
effect of good CSF permeability of fluconazole
useful in meningitis
fluconazole is mainly useful in __
candidal cystitis/candiduria
mucocutaneous candidiasis
posaconazole use
prophylactic for fungal infection in chemotherapy
echinocandins mechanism of action
inhibition of 1,3-beta glucan synthesis
capsofungin (echinocandin) use
disseminated and mucocutaneous candida infection
griseofulvin mechanism of action
binds to microtubules and prevents spindle formation, inhibition of fungal mitosis
griseofulvin adverse effect
disulfiram like reaction
terbinafine mechanism of action
inhibition of squalene epoxidase
terbinafine main use
onchomycosis
metronidazole mechanism of action
inhibition of DNA, RNA, and proteins by creating free radicals
uses of metronidazole and tinidazole
amebiasis
giardiasis
trich. vag.
metronidazole adverse reaction
peripheral neuropathy
disulfiram like reaction
iodoquinol treats what types of infections
luminal amebicide
amebic liver disease drug
chloroquine
adverse effect of emetine
cardiotoxicity
drug for asymptomatic E. histolytica cyst carriers
paromomycin/iodoquinol
drug for mild-severe intestinal amoebiasis E. histolytica
metronidazole/tinidazole with paromomycin/iodoquinol
drug for amebic liver abscess
metronidazole/tinidazole with chloroquine+paromomycin
DOC for t. gondii toxoplasmosis
pyrimethamine+sulfadiazine
DOC in pregnancy for toxoplasmosis T. gondii instead of pyrimethamine+sulfadiazine
spiramycin
DOC for early T. brucei/W. African trypanosomiasis
pentamidine
DOC for advanced E. African trypanosomiasis
melarsoprol
adverse reaction of melarsoprol
fatal reactive encephalopathy
drug for early or late W. African trypanosomiasis
flexinidazole
DOC for blood schizonticide anti-malarial
chloroquine
DOC for tissue schizonticide radial cure of P. ovale and P. vivax
primaquine/tafenoquine
DOC for malarial prophylactic
chloroquine
DOC for malaria in chloroquine reistant areas
mefloquine
DOC for malaria in multi drug resistant area
doxycycline
chloroquine mechanism of action
inhibition of heme polymerase
mechanism of chloroquine resistance
mutation of PfCRT gene–>decrease in efflux of the drug from the parasite
chloroquine adverse effect
visual disturbance (retinal damage)
drug of choice in chloroquine resistant and multidrug resistant P. falciparum
Artesunate
quinine adverse effect
cinchonism (tinnitus, vertigo)
mefloquine adverse effects
psychosis
seizures
pyrimethamine+sulfadoxine adverse reaction
megaloblastic anemia
artemisinin mechanism of action
production of free radicals
primaquine+tafenoquine adverse reaction
hemolysis in G6PD deficient
drug for visceral, mucocutaneous, and cutaneous leishmaniasis
sodium stibogluconate
albendazole, pyrantel palmoate, ivermectin, praziquantal, and diethylcarbamezine (DEC) are all what kind of drugs
antihelmintic
albendazole mechanism of action
inhibition of microtubule synthesis
inhibition of glucose uptake
*both lead to paralysis of the parasite
DOC for hydatid cystic disease, cysticercosis, and neurocysticercosis
albendazole
mechanism of action of pyrantel palmoate
enhance release of ACh
inhibit AChE
depolarize neuromuscular blocker
*produces spastic paralysis
DOC for onchocerca volvulus (river blindness) and strongyloidiasis
ivermectin
ivermectin adverse reaction
Mazotti-like reaction (an allergic reaction to dying microfilariae)
DOC for filariasis and tropical eosinophilia
diethylcarbamazine (DEC)
diethylcarbamazine (DEC) mechanism of action
modifies surface area proteins making them more prone to host cell apoptosis
praziquantel is the drug of choice for __ and __
flukes (trematodes)
cestodes (tapeworms)
what is administered after use of niclosamide
laxative
unfractionated heparin mechanism of action
binds and activates antithrombin III which then inactivates factor IIa and Xa
low molecular weight heparin mechanism of action
binds and activates antithrombin III which then in activates factor Xa
how is unfractionated heparin monitored
PTT
when is unfractionated heparin preferred over low molecular weight heparin
acute conditions due to its rapid onset
*ex: unstable angine, MI
when is low molecular weight heparin preferred over unfractionated heparin
to prevent a DVT or PE during prolonged bed rest, surgery, or fracture
how can excessive bleeding with heparin activity be reversed
use of protamine sulfate
adverse effects of heparin
heparin induced thrombocytopenia (HIT)
inhibition of aldosterone synthesis
osteoporosis
what occurs in heparin induced thrombocytopenia (HIT)
heparin, platelet factor 4, and Ab immune complex reduce the number of platelets
what is the mechanism of action of fondaparinux
inhibition of factor Xa by antithrombin III
warfarin mechanism of actions
inhibition of vitamin K epoxide reductase–>inhibition of synthesis of vitamin K clotting factors and protein C+S
how is warfarin monitored
PT or international normalized ratio (INR)
warfarin adverse reaction
skin necrosis
how is excess bleeding with warfarin reduced
IV administration of vitamin K
what type of drug is dabigatran
direct acting oral thrombin inhibitor
what type of drug is rivaroxaban
direct acting oral factor Xa inhibitor
rivaroxaban is used for treatment of what
PE, DVT, atrial fibrillation
andexanet alpha use
reversal of life threatening bleeding due to a factor Xa inhibitor
drug for non-valvular Afib
dabigatran
fibrinolytic drugs mechanism of action
converts plasminogen to plasmin
plasmin degrades fibrin and fibrinogen causing clot dissolution
drug for use in acute ischemic stroke
recombinant t-PA
aspirin mechanism of action
inhibition of COX-1
ticagrelor and cangrelor are both what class of drugs
antiplatelet
dipyridamole mechanism of action
inhibition of phosphodiesterase
inhibition of inactivation of cAMP
opioid analgesics mechanism of action
inhibition of pain transmitting neurons (ascending pain pathway) and activation of descending pain modulating pathway
morphine is metabolized to M6G and M3G. what is M3G adverse effect
seizures
adverse reactions of opioid analgesics
respiratory depression
pinpoint pupils
CTZ center stimulation
orthostatic hypotension
constipation
what drug is used in dyspnea in pulmonary edema
IV morphine
meperidine effect
antimuscarinic–>tachycardia
pentazocine effect
stimulate sympathetic NS
what opioid drug is preferred over morphine for labor pain
meperidine
what opioid is used for shivering
meperidine
triad of acute opioid poisoning
pinpoint pupils
respiratory depression
coma
treatment for opioid poisoning
naloxone
drug used for opioid withdrawal and detoxification symptoms
buprenorphine with naloxone
opioid analgesic contradictions
head injury
undiagnosed abdominal pain
during labor
__ is used as substitution therapy of opioid dependence patients
methadone
effect of meperidine use with MOA
serotonin syndrome
tramadol mechanism of action
inhibition of reuptake of NE and serotonin
use of tramadol
post-operative pain
difference between naloxone and naltrexone in terms of duration of action
naloxone- short half life
naltrexone- long half life
migraine prophylaxis drugs
methylprednisolone
onabotulinumtoxin A
triptan action
terminate acute attack of migraine
triptan mechanism of action
inhibition of vasodilating neurotransmitters
5-HT receptor agonists
adverse effect of triptan migraine drugs
coronary vasospasm
DOC for acute migraine attacks
sumatriptan
addictive drugs act on what system
mesolimbic dopamine
symptoms of nicotine withdrawal
irritability
anxiety
restlessness
difficulty concentrating
HA
insomnia
nicotine treatment to reduce craving and assist in symptoms of withdrawal
bupropion and clonidine
amphetamine mechanism of action
increase the release of NE, dopamine, and serotonin
chronic use of phencyclidine (PCP) effects
delusions
hallucinations
symptoms of LSD usage
impaired rational decision
dronabinol and nabilone are what class of drug
cannabinoides
dronabinol and nabilone can be used as a __ stimulant
appetite
what type of drug is phenytoin
antiepileptic
pharmokinetics of phenytoin
at low plasma concentration= 1st order kinetics
at higher therapeutic concentration= 0 order kinetics
adverse effects of phenytoin
ataxia, nystagmus, diplopia, vertigo
gingival hyperplasia
hirsutism
carbamazepine mechanism of action
prolongs inactivatd state of Na+ channels
what antiepileptic drug can be used for maniac depressive psychosis
carbamazepine
adverse effects of carbamazepine
agranulocytosis
spina bifida if taken during pregnancy
Steven Johnson syndrome
what allele is at increased risk of Steven Johnson syndrome
HLA 15:02
sodium valproate antiepileptic mechanism of action
blocks T type Ca2+ channels
inhibits GABA transaminase
prolongs inactivation of Na+ channel
adverse effects of sodium valproate
hepatotoxicity
pancreatitis
spina bifida if taken during pregnancy
a mutation in what gene increases the risk of developing fatal sodium valproate hepatotoxicity
POLG
what type of drug is ethosuxmide
anticonvulsant
ethosuximide mechanism of action
inhibition of T-type Ca2+ channels in thalamocortical neurons
ethosuximide is used for what type of seizures
absence (especially in kids)
what type of drug is lamotrigine
anti-convulsant
lamotrigine mechanism of action
blocks Na+ and Ca2+ channels
adverse effect of lamotrigine
Steven Johnson syndrome
what type of drug is topiramate
anticonvulsant
adverse effects of topiramate
loss of appetite weight loss
cognitive impairment
what type of drug is levetiracetam
antiepileptic
levetiracetam mechanism of action
reduces the release of glutamate
gabapentin and pregabalin use
antiepileptic
gabapentin and pregabalin mechanism of action
binds to alpha2delta subunit of P/Q type Ca2+ channel decreasing the release of glutamate
besides seizures, gabapentin and pregabalin can be used for __
neuropathic pain
felbamate use
anticonvulsant
felbamate mechanism of action
blocks NMDA receptors
vigabatrin mechanism of action
irreversible inhibitor of GABA transaminase
use of vigabatrin
infantile spasm (West syndrome)
vigabatrin adverse effect
retinal damage
tiagabine mechanism of action
blocks uptake of GABA into presynaptic neurons
zonisamide adverse effects
inhibition of carbonic anhydrase
zonisamide adverse effect
Steven Johnson syndrome
drug of choice for status epilepticus
benzodiazepines (diazepam or lorazepam)
if benzodiazepines don’t work for status epilepticus, what is the next drug of choice
fosphenytoin
benzodiazepines preferred in the elderly
lorazepam
oxazepam
temazepam
why are lorazepam, oxazepam, and temazepam benzodiazepines preferred in the elderly
they have no 1st phase metabolism
adverse effects of benzodiazepines
daytime drowsiness
respiratory depression
benzodiazepine respiratory depression is exacerbated in patients with ___
obstructive sleep apnea
do short or long acting benzodiazepines cause more abrupt and sever
short
what drug class can cause floppy baby syndrome
benzodiazepines
drug used for benzodiazepine toxicity
flumazenil
Z drug (zolpidem, zaleplon, zopiclone) mechanism of action
act on BZ1 receptor (GABA A receptor)
main use of Z drugs instead of benzodiazepines
treat insomnia
barbiturates mechanism of action
increase duration of GABA A gated chloride channel opening
benzodiazepines or barbiturates to treat neonatal jaundice
barbiturates
barbiturate use contraindicated in __
acute intermittent porphyria
treatment for acute barbiturate poisoning
forced alkaline diuresis
buspirone drug class
anti-anxiety