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124 Cards in this Set
- Front
- Back
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methohexital, thiamylal, thiopental
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- ultra short (15-30min) barbiturates
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pentobarbital, secobarbital
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- short acting (2-4h) barbiturates
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amobarbital, butalbital, butabarbital, aprobarbital
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- intermediate (4-5h) acting barbiturates
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phenobarbital, mephobarbital
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- long acting barbiturates (6-8+h)
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ramelteon
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- melatonin receptor agonist
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flumazenil
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- benzodiazepine antagonist
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zaleplon, zolpidem, eszopiclone
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- GABA agonists
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phenytoin
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- hydantoin
- usage dependent Na+ channel blockade (plus some increase in GABA release) |
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mephenytoin
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- hydantoin anticonvulsant, lower minor toxicities, more serious toxicities
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ethotoin
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- low toxicity, low efficacy hydantoin
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carbamazepine
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- Na+ channel blockade (binds inactive)
- all types of seizures (except absence) |
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oxcarbazepine
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- Na+ channel blockade
- less hypersensitivity than carbamazepine |
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barbiturates (as anticonvulsants)
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- increase GABA affinity at receptor
- some GLU blockade at AMPA receptor - blockage of VGCa++ channel (high concentrations) |
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primidone
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- active metabolites are PEMA and phenobarbital
- Na+ channel blockade |
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valproate
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- blocks Na+ Channels (partial)
- blocks NMDA receptor - good for absence (?) |
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succinamides
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- block T-type Ca++ channels
- absence |
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lamotrigine
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- Na+ channel inhibition
- VG-Ca++ (P/Q) |
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felbamate
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- GABAa potentiator
- usage dependent NMDA blockade - aplastic anemia and hepatitis |
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topiramate
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- Na+ channels
- GABA - GLU receptors - cognitive slowing, but good for varying types of seizures |
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gabapentin/pregabalin
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- analogues of GABA
- bind a2d subunit of N type VG-Ca++ (presynapitc) and inhibit Glu release - partial, and neuropathic pain |
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tiagabine
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- GABA reuptake inhibitor
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levetiracetam
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- SV2A blocker (Glu release inhibitor)
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vigabatrin
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- indirect GABA agonist (prevents degradation by inhibiting gaba aminotransferase)
- VISION LOSS |
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lacosamide
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- binds to CRMP-2 and blocks BDNF and NT3 on axonal/dendritic growth
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zonisamide
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- effect on Na+ and Ca++ channels
- no GABA effect - inhibits carbonic anhydrase |
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levodopa
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- D agonist (small amt. reach CNS)
- ADV: diskynesias, behavioral disturbances |
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carbidopa
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- DOPA decarboxylase inhibitor
- greatly increases amt. of L-dopa reaching CNS, reducing side effects |
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amantadine/symmetrel (for PD)
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- indirect DA agonist
- only short duration of effect (weeks) |
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bromocriptine
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- D2 agonist for early stage parkinsons
- first dose CV collapse |
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pergolide
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- D1 and D2 agonist for early stage PD
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ropinirole/pramipexole
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- D2, D2/D3 agonists
- high degree of CNS disturbances |
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selegiline
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- MAO-B selective (at low doses)
- reversible inhibition -useful early (or late with levodopa) |
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rasagiline
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- irreversible inhibition of MAOB
- may have neuroprotective properties |
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tolcapone
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- irreversible COMT inhibitor in brain and periphery
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entcapone
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- reversible COMT inhibitor (mainly in liver, little CNS penetration)
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benztropine mesylate, trihexyphenidyl, ethopropazine
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- anticholinergics for PD
- wide SE profile - possible use for Tx of traditional antipsychotic symptoms |
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apomorphine
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- selective D2 agonist (post-synaptic)
- used for "off-period" rescue for PD - pretreat with antiemetic and up to 3 months after |
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tetrabenazine
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- depletes DA, NE, 5HT from vesicular transporters
- brief relief of Huntington's - TX of movement disorders |
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chlorpromazine
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- typical antipsychotic
- a1/5HT blocker - hypotension |
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haloperidol
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- D2 blocker
- typical antipsychotic |
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clozapine
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- 5HT2a blocker (others, but low D2 blockade)
- IND: treatment resistant schiz - SOMA |
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olanzapine
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- 5HT2a, DA, muscarinic blockade
- weight gain (main), sedation, dry mouth |
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risperidone
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- 5HT2a blocker
- popular first line - EPS above 6mg and hyperprolactinemia |
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quetiapine
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- 5HT2a blocker
- no EPS at any dose - 200mg BID |
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ziprasidone
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- D2, 5HT2a blocker
- QT prolongation |
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aripiprazole
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- DA modulator
- first line |
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lithium
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- inhibits recycling of inositol substrates
- toxicity difficult to avoid |
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trazodone/nefazodone
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- 5HT2a (presynaptic) antagonists for depression
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tranylcypromine, phenelzine
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- MAOI's (depression)
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tacrine
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- ACHEI (reversible) for AD
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donepezil
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- reversible ACHEI for AD
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galantamine
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- reversible ACHEI inhibitor
- allosteric effect on nicotinic receptors good for AD |
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rivastigmine
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- pseudo-irreversible inhibition of ACHE
- short half-life, long duration |
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memantine
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- non-competative NMDA blokade for AD
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lodoxamide, pemirolast
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- ophthalmic mast cell stabilizers
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buspirone
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- 5HT1a agonist (anxiolytic)
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sumatriptan and congeners
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- 5HT1D/B agonists (triptans)
- Tx: migraines |
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tegaserod
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- 5HT4 partial agonist
- CPIBS |
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isoproterenol
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- non-selective B1/2 agonistm
- bronchodilation but also increased HR/BP |
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metaproterenol
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- specific B2 agonist for asthma
- resistant to COMT |
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tertbutaline, albuterol, levalbuterol, metaproterenol, pirbuterol, bitolterol (prodrug)
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- B2 agonist
- resistant to COMT - short (2-6 hour) duration |
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salmeterol, formoterol
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- B2 agonist
- resistant to COMT - delayed onset, long duration |
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ipratropium bromide
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- M3 receptor antagonist, short acting
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tiotropium
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- M3 receptor antagonist, long acting (higher affinity)
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glucocorticoids (asthma)
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- inhibitors of PLA2
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zileuton
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- 5-lipoxygenase inhibitor, prevents leukotriene formation
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zafirlukast
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- inhibits cysteinyl leukotriene receptor
- peptide w/ drug (warfarin) interactions |
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montelukast
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- non-peptide cysteinyl leukotriene receptor antagonist
- non-peptide - less drug interaction |
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omalizumab
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- humanized monoclonal antibody (IgG) which blocks IgE receptor
- Tx: steroid resistant asthma |
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theophylline
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- methylxanthine
- phosphodiesterase inhibitor (nonselective) - Tx: asthma (not first line) |
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indole NSAIDS
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- indomethacin (high SE)
- suldinac - etodolac - pharmacologically similar to salicylates |
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fenamates
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- mefenamic acid, meclofenamate
- not 1st line, high GI upset |
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propionic acid derivatives
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- profens + naproxen
- beter tolerance, some reduction of antihypertensives |
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enolic acid NSAIDS
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- oxicams
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tolmetin
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- NSAID
- better tolerance than aspirin - highly protein bound |
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diclofenac
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- NSAID
- leads to HTX similarly to APAP |
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nabumetone
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- misc. NSAID
- somewhat cox 2 selective |
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gold
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- inhibitor of mononuclear phagocytes and T cell function in RA
- may cause blue skin/mucous membranes |
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leflunomide
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- dihydroorotate dehydrogenase inhibitor for RA
- induces p53 and inhibits pyrimidine synthesis in lymphocytes - teratogen, SJS |
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etanercept
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- recombinant human soluble receptor for TNFa
- Tx: RA |
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infliximab
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- monoclonal antibody for TNFa
- RA, Crohn's - ADV - respiratory infections - sub Q |
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adalimumab
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- monoclonal antibody for TNFa
- ADV - respiratory infections - sub Q |
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anakinra
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- recombinant interleukin 1 receptor antagonist
- RA - ADV: low WBC count |
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abatacept
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- soluble fusion protein consisting of extracellular domain of T-lymphocyte associated antigen (CTLA-4) linked to immunoglobulin IgG1
- inhibits T-activation, proliferation, and production of TNFa, interferon-Y, IL-6, and IL-2 - do not use with TNF-a antagonist (infections) |
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penicillamine
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- metal chelator - thought to be relation between Cu and RA
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hydroxychloroquine
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- antimalarial agent for RA
- ocular toxicity |
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colchicine
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- inhibits granulocyte response to urate crystals by inhibiting tubulin function in mitotic spindles
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allopurinol
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- XO inhibitor
- antihyperuricemic |
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probenecid
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- uricosuric agent
- increases secretion of uric acid, decreases secretion of everything else |
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somatropin
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- recombinant human GH
- receptor activation produces IGF-1 |
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mecasermin
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- recombinant IGF-1
- used when patients don't respond to GH |
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octreotide, lanreotide
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- somatostatin analog
- inhbits GH production, and others - Tx: acromegaly, tumor secreting hormonnes |
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pegvisomant
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- pegylated rhGH which is partial agonist at receptor
- reduces effects of excess GH - Tx: acromegaly |
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FSH analogs (itropins)
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- controlled ovulation hyperstimulation
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LH analogs
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- used to stimulate ovulation
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leuprolide, goserelin, nafarelin
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- GnRH agonists
- increases FSH and LH (short term), decreases (long term) - also TX advanced prostate cancer |
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____-relix
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- GnRH antagonists
- reduces LH and FSH production - prevention of premature LH surges during COH, or advanced prostate cancer |
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bromocriptine, cabergoline
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- ergot D2 agonists for hyperprolactinemia, PD
- less robust than pramipexole, ropinirole |
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oxytocin
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- induction of labor, control of uterine hemorrhage after delivery
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desmmopressin/vasopressin
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- decrease secretion of water
- Tx: diabetes insipidus, von Willebrand disease |
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conivaptan/tolvaptan
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- vasopressin receptor antagonists
- increase water secretion in hyponatremia |
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methimazole
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- thyroid peroxidase inhibitor
- Tx: hyperthyroidism |
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propylthiouracil (PTU)
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- thyroid preoxidase inhibitor
- also inhibits T3-->T4 in periphery - Tx: hyperthyroidism |
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iodide
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- in high concentrations, inhibits iodide uptake
- radioactive I given as alternative to surgery |
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mitotane
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- DDT analog, toxic to adrenocortical mitochondria
- compassionate care of adrenal carcinoma |
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aminoglutethimide
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- desmolase inhibitor
- blocks production of all hormonally active steroids - Tx: cushings |
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metyrapone
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- inhibits cortisol synthesis
- commonly used to test adrenal function, if normal, ACTH will increase |
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trilostane
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- inhibits cortisol and aldosterone synthesis
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DHEA
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- chronic fatigue syndrome, hypoaldosteronism
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clomiphene
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- SERM
- partial estrogen agonist - used to antagonize estrogen feedback to release FSH and LH |
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mifepristone
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- competitive progesterone antagonist
- abortifacent |
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danazol
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- weak progesterone, testosterone, glucocorticoid agonist, used to suppress mid cycle FSH and LH surges without changing basal levels
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fluvestrant
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- estrogen receptor antagonist
- cancer |
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meperidine
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- Mu opioid agonist
- nor-metabolite is CNS toxic |
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pentazocine
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- partial Mu, full K agonist
- no respiratory depression |
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butorphanol
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- partial Mu, K agonist
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nalbuphine
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- Mu/K agonist equipotent to morphine
- respiratory depression ceiling at 30mg |
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buprenorphine
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- partial Mu agonist, full K antagonist
- very high affinity/long half life |
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tramadol
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- Mu opioid agonist
- also inhibits SERT and NET (seizures) |
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naloxone
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- opioid antagonist
- short duration - not orally active |
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naltrexone
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- opioid antagonist, long acting, orally active
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mescaline, MDMA
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- hallucinogen (amphetamine like)
- 5HT indirect agonist |
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LSD, psilocybin (mushrooms), tryptamines, bufotenine (toads)
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- serotonin-like hallucinogens (direct 5HT agonists)
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ketamine, PCP
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- dissociative hallucinogens
- usage dependent NMDA blokade |
