Term
|
Definition
Indirect Acting Sympathomimetic: Displaces stored Catecholamines w/i Nerve Enters CNS more readily than Ephedrine D isomer more potent Actions mediated thru release of NorEpi and to some extent DA |
|
|
Term
|
Definition
Indirect Acting SympMimeSimilar to Amphetamine but higher ratio of CNS to PNS action |
|
|
Term
|
Definition
Mixed acting Sympathomimetic High bio-availability and long duration weak base, so excretion is accelerated by adification of urine. activates B receptors |
|
|
Term
|
Definition
Indirect SympMime. byproduct of Tyr metab. found in cheese. metabolized by MAO, mostly MAO-A, in liver = low oral bio-availability. Action similar to NE. effect intensified with MAO inhibitors |
|
|
Term
|
Definition
Indirect Acting SympMime Psychostimulate for Narcolepsy MOA: inhibits NE & DA transporters Increases NE, DA, SER, and GLU Decreases GABA |
|
|
Term
|
Definition
Indirect Acting SympMime Racemic Amphetamine variant: blocks NE and DA reuptake For ADHD: short, med, and long acting |
|
|
Term
Indirect Acting Sympahtomimtics |
|
Definition
2 MOA 1) Enter Sym Nerve & displace Catechol 2) Inhibit reuptake of released nt's thru NET |
|
|
Term
|
Definition
NON STIMULANT inhibits NET w/ NO DA EFFECT No DA effect = less abuse and no increase in psychomotor activity used with ADHD Metab by CYP2D6. avoid CYP inhibitors paroxetine and fluoxetine Side Fx: GI, Orthostatic tachycardia. this side effect is seen with most NET blockers due to NE uptake in heart |
|
|
Term
|
Definition
Inhibits NET Enters CNS w/ short yet intense Amphetamine-like actions Main MOA: inhib DA uptake in pleasure centers of brain |
|
|
Term
dexmethylphenidate (Focalin) |
|
Definition
d - enatiomer of methylphenidate more pharmacologically active |
|
|
Term
dextroamphetamine (Dexedrine) |
|
Definition
d-enantiomer of amphetamine more biologically active |
|
|
Term
lisdexamfetamine (Vyvanse) |
|
Definition
pro-drug: d-amphetamine covalent bonded to L-Lysine. less abuse and toxicity |
|
|
Term
amphetamine mixed salts (Adderall) |
|
Definition
racemic mixture of amphetamine |
|
|
Term
|
Definition
HTN and possible arrythmia of course mental problems. Avoid use with anti-depressent b/c may increase half life. Contra-idx with closed angle glaucoma |
|
|
Term
|
Definition
Atypical Antipsychotic D2 partial agonist = acts as antagonist to endogenous DA very low EPS |
|
|
Term
atypical antipsychotic MOA |
|
Definition
For schizophrenia: pos and neg sx's Binds D2 receptors with low affinity Binds 5HT 2A and 1A receptors Total affect is increased DA release in Striatum, with few Parkinson like Side FX |
|
|
Term
|
Definition
SSRI: blocks SERT for depression, anxiety, OCD, eating disorder Side Fx: sexual dysfunction. Can inhibit CYP2D6 and CYP3A4 |
|
|
Term
|
Definition
SSRI simlilar to fluoxetine |
|
|
Term
|
Definition
SSRI similar to fluoxetine |
|
|
Term
|
Definition
SSRI similar to fluoxetine inhibits CYP2D6 |
|
|
Term
|
Definition
SSRI S enantiomer of citalopram similar to fluoxetine |
|
|
Term
|
Definition
|
|
Term
|
Definition
SNRI: moderate blockade of NET and SERT for major depression and chronic pain Tox: anticholinergic, sedation, HTN |
|
|
Term
|
Definition
SNRI similar to venlafaxine CYP2D6 inhibition |
|
|
Term
desvenlafaxine (Pristique) |
|
Definition
phase II metabolite of venlafaxine CYP2D6 inhibition |
|
|
Term
|
Definition
TCA only blocks NE reuptake blocks HIS, muscarinic and Alpha receptors |
|
|
Term
|
Definition
TCA Blocks 5HT and NE reuptake blocks HIS, muscarinic and Alpha receptors |
|
|
Term
|
Definition
TCA blocks 5HT and NE reuptake blocks HIS, muscarinic and Alpha recpetors |
|
|
Term
|
Definition
TCA Blocks 5HT and NE reuptake blocks HIS, muscarinic and Alpha receptors |
|
|
Term
|
Definition
Due to Ca++ and Na++ VGC blocking, can induce cardio-toxicity |
|
|
Term
|
Definition
Herbal supplement sedative/hypnotic for insomnia Combined with St. Johns wort for anxiety no known contra indications |
|
|
Term
|
Definition
Benzodiazepine GABA A agonist combined with alcohol = Date Rape Drug can lead to tolerance and dependence withdrawals can be fatal |
|
|
Term
|
Definition
cough suppressant in high doses produces dissociative effects Blocks NMDA-type glutamte receptors Avoid taking with MOA-I Has side effect of blocking SERT |
|
|
Term
Buprenorphine (Subutex) (Suboxone: paired with naloxone) |
|
Definition
Opioid used for opioid withdrawls little respiratory depression Sub-lingual tablets partial agonist of mu opioid receptor Higher binding affinity and longer duration to mu receptor than other opioids kappa opioid receptor antagonist= induces positive mood |
|
|
Term
|
Definition
Oral tx of tobacco dependence partial agonist to nicotinic receptors high affinity than nicotine binding of this receptor leads to DA release Absorbed in GI Side Effects: nausea Competes with H2 agonist cimetidine for clearance more effective than bupropion may exacerbate pre-existing psychiatric illnesses |
|
|
Term
|
Definition
Oral; Alzhiemers and vascular dementia
non-competitive NMDA glutamate antagonist: directly blocks ion channel channel; channel must be open for drug to enter and exert effect
fast on - off rate = differs from other NMDA blockers
blocks moderately high levels of Glutamate activity as seen Alz but not VERY HIGH levels of Glutamate as seen with intentional neuron firing
no adverse psychotic side effects
antagonist of excitatory ionotropic 5HT3 receptor excretion reduced with alkaline urine
combo'd with ACHE inhibitor Donepezil
Avoid use with other NMDA antagonist |
|
|
Term
|
Definition
oral ACHE inhibitor for Alzheimer combo'd with memantine high CNS entry metabolized by CYTP450 Side FX: nausea, vomiting |
|
|
Term
|
Definition
oral ACHE inhibitor of Alzheimer High CNS entry metabolized by CYTP450 Side FX: nausea, vomiting |
|
|
Term
|
Definition
oral ACHE inhibitor for Alzheimer high CNS entry metabolized by CYTP450 Side FX: nausea, vomiting |
|
|
Term
St. Johns wort (hypericum perforatum) |
|
Definition
Tx for depression MAO-A and -B inhibitor at high doses Downregulate cortical Beta adrenoceptors Upregulate 5-HT2 expression hypericin extract used to treat cancer and HIV to to photoactivity |
|
|
Term
|
Definition
Atypical Anti-Psychotic Inverse 5HT-2A Agonist : block constitutive activity Blocks His, Musc, and Alpha recpetors side fx: agranulocytosis, diabetes, hypercholesterolemia, weight gain |
|
|
Term
Typical Anti-Psychotics (neuroleptics) |
|
Definition
Alter 5HT2A more than D2 block D2 receptors = Increase cAMP Tx: Schizo, mania, Tourettes Side Effects: EPS, galactorrhea, also blocks His, alpha, and muscarinic receptors NMS, tardive dyskinesia |
|
|
Term
|
Definition
Butyrophenone derivative very potent: bioavailabilty 65% D2>a1>D4>5HT2A>D1>H1 most used Typical antipsychotic EPS |
|
|
Term
|
Definition
Atypical AntiPSY 5-HT2A > D2 rapidly converted to 9-hydroxyrisperidone (paliperidone) |
|
|
Term
mesolimbic-mesocortical pathway |
|
Definition
Substansia nigra to limbic system and neocortex |
|
|
Term
|
Definition
S. Nigra to dorsal striatum (caudate and putamen) voluntary movement blocking D2 in pathway results in EPS |
|
|
Term
|
Definition
arcuate nuclei and periventricular neurons release DA into pituitary portal circulation Da released here inhibits prolactin secretion from Anterior Pituitary |
|
|
Term
medullary-periventricular |
|
Definition
motor nucleus of Vagus Dopaminergic system |
|
|
Term
|
Definition
tx of HSV-1, HSV-2, and VZV more potent against HSV than VZV Phosphorylated 3 times for activation: 1st by virus thymidine kinase competes with deoxyGTP and is a chain terminator Oral and IV with renal excretion Tx of choice for HSV encephalitis MOR: thymidine kinase mutation |
|
|
Term
|
Definition
Nonsedative for partial and generlized Tonic-Clonic seizure Alters Na, K, and Ca conductance Keeps Na channels inactivated Decreases Glutamate release, Increases GABA release GI absorption, bound to plasma proteins metabolism thru 1st order kinetics Once theraputic value reached, metabolism is maxed and small change in dose is big change is plasma concentration Tox: gingival hyperplasia, nystagmus, interfere w/ Vit D metabolism, |
|
|
Term
|
Definition
Anticonvulsant Tricycleic antidepressent for bipolar blocks Na channels = blocks neuron firing
Older patients may not tolerate given w/ meals for better toleration 70% bound to plasma proteins
Enzyme inducing properties: increases rate of metabolism for itself and other drugs
Tox: diplopia and ataxia. aplastic anemia, agranulocytosis, leukopenia |
|
|
Term
|
Definition
Anticonvulsant pheno, mepho, metha - barbitols Change in acid-base balance affects ionized concentration |
|
|
Term
|
Definition
Benzodiazepine for Tonic-Clonic Sz and Status epilepticus Increases GABA affinity for GABA-A IV or Rectal |
|
|
Term
|
Definition
Long acting Benzo; very potent Absence seizure, myclonic seizure sedation is prominent |
|
|
Term
|
Definition
Allosterically binds GABA-A Increases GABA affinity and thus increases number of times channel opens, Cl enters, and neuron hyperpolarizes |
|
|
Term
|
Definition
Inhibit GABA uptake in neurons and glia Inhibits GAT-1 thus increasing GABA in forebrain and hippocampus Tx of partial seizure side fx: dizzyness, tremor, seizures protein bound in plasma oxidized in liver by CYP3A |
|
|
Term
|
Definition
blocks VGC Na Channels potentiates GABA signals and supresses Glutamate
Tx of partial and generalized tonic-clonic seizure, Lennox Gastaut Syndrome, migranes
Side FX: myopia, glaucoma
Oral |
|
|
Term
|
Definition
sulfonamide derivative Na channel blocker partial and generalized seizures Side Fx: drowsiness, skin rash |
|
|
Term
|
Definition
succinimide Blocks T-type Ca channels in thalamic neurons Tx for absence seizures Metabolized by hydroxylation adminisstration with valproic acid decreases ethosuximide metabolism |
|
|
Term
|
Definition
Bipolar, Anti-seizure: absence seizure
MOA unclear: inhibits histone deacetylase
displaces phenytoin from plasma prt, inhibits metab of phenobarbital, phenytoin, carbamzepine and can result in coma/stupor
Decreases clearance of lamotrigine
Hepatotoxic |
|
|
Term
|
Definition
metabo to 1)phenobarbital(thru oxidation). has low clearance 2) and PEMA MOA more like phenytoin Tx of partial and generalized tonic-clonic seizure start low dose and steadily increase side fx same as phenobarbital |
|
|
Term
|
Definition
Anti-seizure with anti folate side effect inactivates Na channels, Ca channels (N- and P/Q type) decreases Glutamate release used as add-on therapy mostly also for bipolar treatment |
|
|
Term
|
Definition
GABA analog effective for partial seizure. does not direct act on GABA receptors, but increases GABA release transported to brain by L-aa transporter bind voltage-gated Ca channel this decreases glutamate release also for treatment of neuropathic pain not metabolized, excreted unchanged |
|
|
Term
|
Definition
Adjunctive tx for partial seizures GABA analog binds VG-Ca channels and decreases glutamate release approved for nueropathic pain not metabolized and excreted unchanged |
|
|
Term
|
Definition
Opioid full agonist at μ receptors in CNS; principle effects include: analgesia, euphoria, sedation, and respiratory distress; siginificant first-pass effect poppy seed extract |
|
|
Term
|
Definition
Opioid potent and fast acting; more effective in relieving severe chronic pain when given IM |
|
|
Term
|
Definition
partial agonist of mu receptor synthesized from morphine large first pass effect cough suppressant |
|
|
Term
|
Definition
w/ acetominophen= Percocet w/ asprin = Percodan |
|
|
Term
|
Definition
w/ acetominophen = Vicodin or Lortab w/ ibuprofen = Vicoprofen |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
synthetic opioid highly lipophilic and slowly metabolized by CYP3A4 so can accumulate in tissue |
|
|
Term
|
Definition
older opioid, significant antimuscarinic effects and can block 5-HT reuptake Side FX: tachycardia common abuse by health care professionals |
|
|
Term
|
Definition
opioid low analgesic activity, but analgesic effect is additive |
|
|
Term
|
Definition
weak mu opioid receptor agonist/blocks 5-HT reuptake/ antimuscarinic
for patients w/ epilepsy or on seizure drugs; nausea, dizziness; adjunct w/ pure opioid agonists in the treatment of chronic neuropathic pain
Per Wiki: CNS opioid analgesic, for tx of pain. has a wide range of applications, including treatment for restless legs syndrome and fibromyalgia |
|
|
Term
|
Definition
opioid strong kappa opioid receptor agonist/ mu opioid receptor antagonist less respiratory depressant effects but cause dysphoria - limited use |
|
|
Term
|
Definition
kappa opioid receptor agonist/weak mu antagonist or partial agonist |
|
|
Term
|
Definition
kappa opioid receptor agonist/mu opioid receptor partial agonist or antagonist; significant first-pass effect High sedation effect |
|
|
Term
|
Definition
long lasting partial mu opioid receptor agonist also a kappa receptor antagonist; given sublingual, detox for Heroin abusers (alternative for methadone) |
|
|
Term
|
Definition
fast acting mu-antagonist
for opiate OD |
|
|
Term
|
Definition
for migraine serotonin agonists, act on serotonin receptors (5-HT1D) found on small, peripheral nerves that innervate the intracranial vasculature. Causes vasoconstriction. Short duration of action (migraine may last longer) but first line |
|
|
Term
|
Definition
ergot alkaloid: stimulates the alpha adrenergic receptors and DA receptors, producing peripheral vasoconstriction and decreased blood flow; exhibits serotonin antagonistic properties, caffeine enhances vasoconstrictive effects |
|
|
Term
|
Definition
ergot alkaloid: safer alternative to ergotamine Ineffective in treating activce migraine episodes, No longer available in USA |
|
|
Term
|
Definition
activate μ receptors for inhibitory G proteins on GABA neurons of VTA, resulting in the disinhibition of dopamine neurons. Thus opioids bind to inhibitory GPCRs and lead to decreased adenyly cyclase severe withdrawls |
|
|
Term
|
Definition
"retrograde messengers" disinhibition of dopamine neurons, mainly by presynaptic inhibition of GABA neurons in the VTA |
|
|
Term
|
Definition
weak GABA-B agonist; GHB agonist
at high doses GHB hyperpolarizes dopamine neurons to extent of no dopamine release
used as anticraving compound for other drugs
Used as date rape drug; creates euphoria
street drug name: liquid X (as in raves)
per wiki: GHB has been used in a medical setting as a general anesthetic, to treat conditions such as insomnia, narcolepsy, and alcoholism |
|
|
Term
|
Definition
increases dopamine release in mesolimbic reward system by way of receptors that include: GABAA receptors, Kir3/GIRK channels, glycine receptor, NMDA receptor, 5-HT3 receptor |
|
|
Term
|
Definition
nicotine is a selective agonist of nicotine acetylcholine receptor (nAChR), which are on dopamin neurons in the VTA. Nicotine excites projection neurons that release dopamine into nucleus accumbens and the prefrontal cortex |
|
|
Term
benzodiazepines and barbituates |
|
Definition
positive modulators of GABAA receptor, GABA receptors on dopamine neurons of the VTA lack α1, subunit present in GABA neurons. |
|
|
Term
|
Definition
in CNS blocks the uptake of dopamine, noradrenaline, and serotonin through their respective transporters; blocks DAT increasing dopamine concentration in nucleus accumbens |
|
|
Term
3,4 methylenedioxymethamphetamine MDMA |
|
Definition
aka Ecstasy, X, E, Rolls, Thizz Increases neurotransmitter release by reversing transporters; affinity for serotonin transporter (SERT) increases concentration of serotonin but long term use depletes 5HT fosters feelings of intimacy |
|
|
Term
|
Definition
MOA unknown but NO binds to NMDA receptors and fuel addiction
enhance GABA-A receptor function
long term use = white matter lesions |
|
|
Term
ketamine and phencyclidine |
|
Definition
use dependent, noncompetitive antagonism of the NMDA receptor increased BP, impaired memory function, visual alterations, out-of-body experiences. OD =stupor or coma |
|
|
Term
lysergic acid diethylamid: LSD mescaline psilocybin |
|
Definition
fail to stimulate dopamine release (not addictive), increase glutamate release in the cortex, target the 5-HT2A receptor that couples to G protein of the Gq type leads to release of intracellular calcium Repeat use creates tolerance Users experience hallucinations |
|
|
Term
|
Definition
alpha2 adrenergic receptor agonist. longer acting opioid used to suppress withdrawal symptoms. So acutually decreases release of NE from LC. The sudden loss of the opiate is going to cause a surge in NE |
|
|
Term
|
Definition
blocks aldehyde dehydrogenase for alcohol abuse |
|
|
Term
|
Definition
long acting mu opioid receptor antagonist; blocks effects of illicit opioids
Stops the urge to drink alcohol |
|
|
Term
|
Definition
GABA analog; antagonist of NMDA glutamate receptors decreases drinking frequency, relapse-low potential for abuse and few SE; MAO unknown-may modulate NMDAR fxn |
|
|
Term
|
Definition
slow-acting agonist of μ opioid receptor, acute effects similar to morphine; oral substitution therapy for opioid addicts |
|
|
Term
|
Definition
Indirect-Acting Sympatholytic Blocks VMAT(biogenic amine transporter) ' blocks ability to uptake and store norepi, dopamine, and serotonin in central and peripheral neurons=depletion irreversible (remains bound to membrane for many days). USES: Antipsychotic; Antihypertensive at lower doses(depletion of peripheral amines); lowers BP; Dyskinesias in Huntington's |
|
|
Term
|
Definition
potent anesthetic but relatively weak analgesic; prolongation of the inhibitory chloride ion current after a pulse of GABA release
Side FX: Malig Hyperthermia, hepatitis |
|
|
Term
|
Definition
less potent than halothane, but rapid induction and recovery differences from halothane: fewer arrhythmias, less sensitization of the heart to catecholamines |
|
|
Term
|
Definition
One of first drugs used as Typical Anti-Psychotics blocks D2 receptor, Muscarinic receptor, Histamine blocker and alpha receptor to some extent Tx of shcizophrenia (positive symptoms), Mania of Bi-polar |
|
|
Term
|
Definition
Typical Anti-Psychotic Blocks: D2, alpha, muscarinic receptors QT prolongation |
|
|
Term
|
Definition
IV anesthetic/sedative prolonged use associated with acidosis Liver metabolism via conguation SIGNIFICANTLY LOWERS BP AND HR |
|
|
Term
|
Definition
Carboxylated Imidazole Use: induction of anethesia W/O BP OR HR EFFECTS No analgesic effects so used w/ Opioid Side FX: Pain with Injection, nausea |
|
|
Term
|
Definition
racemic mixture produces a dissociative anesthtic state
S(+) most potent (catatonia, amnesia, analgesia) MOA: block NMDA receptor highly lipophilic only IV anesthetic w/ anesthetic and analgesic properties
CNS stimluate: increases NE and Epi plasma levels
increases ICP; decreases RR
Post-op Psychic phenomena seen
related to PCP |
|
|
Term
|
Definition
Barbitiuate for anesthesia induction
High Lipid Solubility
Rapidly diffuses in and out of Brain (immediate yet short effects)
Myocardial depressant and Respiratory depressant
No affect on ICP so Good for patients with head injuries
use with ECT
barbituates induce ALA synthanse and thus exacerbate acute intermittent porphyria |
|
|
Term
|
Definition
Benzo preanesthetic med for local surgeries
sedative, anxiolytic, and amnestic properties
water soluble but lipid soluble at physiologic pH
side fx: amnesia
rapid onset w/ shorter elimination
flumazenil use to accelerate recovery |
|
|
Term
|
Definition
Fentanyl and droperidol co-administered produce analgeisa and amnesia and combined with NO provide a state referred to as neruoleptanesthsia |
|
|
Term
|
Definition
most commonly used volatile gasses: isolflurane, desflurane, and sevoflurane
NO is important adjuvant to the volatile agents
MOA: direct acting GABA-A agonist (dont need GABA to produce effect like Barb and Benzo do)
also
activate K+ channels and Nicotinic cation channels(possible glycine recptors too)
|
|
|
Term
stages of general anesthesia |
|
Definition
I. analgesia
II. excitement - delirious, may vocalize but amnesic
respiration irreg
III. surgical anesthesia - regular respiration reoccurs. no more apnea
IV. medullary depression - severe CNS depression;
vasomotor and respiratory centers depressed |
|
|
Term
|
Definition
incomplete anesthetic; rapid onset and recovery
MAC greater than 100 = non-analgesic
low solubility in blood = rapidly enters and leaves tissue
|
|
|
Term
|
Definition
rapid onset and recovery; unstable in soda-lime |
|
|
Term
|
Definition
medium rate onset and recovery |
|
|
Term
|
Definition
sedative (anxiolytic) exert a calming effect
degree of CNS depression is minimal
hypnotics produce drowsiness and encourage onset/maintenance of sleep; higher CNS depression
graded dose dependent CNS depression is characteristic of most sedative/hypnotics |
|
|
Term
|
Definition
antagonist of GABA-A benzo binding site
blocks benzo and benzo like hypnotics (Z,Z,esZ)
for Benzo OD
tox: agitation, confusion |
|
|
Term
|
Definition
Partial 5-HT agonist with some D2 binding
Slow onset of anxiolytic effects for GAD
NOT FOR ACUTE ANXIETY/ PANIC ATTACKS
no sedative, hypnotic or euphoric effects
tox: tachy, paresthesia, metablolized by CY3A4 |
|
|
Term
zolpidem, zaleplon, eszopiclone |
|
Definition
Hypnotics that arent benzo but act like benzo
GABA-A alpha-1 subunit specific
absorbed into blood rapidly
Help insomnia but with decreased Stage 3, 4, and REM sleep |
|
|
Term
Beznodiazepine metabolization |
|
Definition
Phase I via CYP3A4
The metabolites then thru conjugated in Phase II rxn and excreted in urine
exceptions: lorazepam and desmethyldiazepam directly conjugated |
|
|
Term
|
Definition
benzo metabolite thats biologically active |
|
|
Term
|
Definition
hypnotic for patients who have difficulty falling asleep
MT1 and MT2 melatonin receptor agonist in the suprachiasmatic nuclei
P.O. with extensive 1st pass effect |
|
|
Term
benztropine and trihexyphenidyl |
|
Definition
CNS Muscarinic antagonist (w/i basal ganglia)
improve tremor and rigidity in PD
little effect w/ bradykenesia
Tx started with low dose, tapered up till desired effect
|
|
|
Term
|
Definition
Tx of Bipolar (esp Manic phase) & reoccurant endogenous depression
MOA: depletes intracelluar inositol and inhibits GSK-3
this inhibits intracellular signaling (IP3 + DAG)
substitutes for Na+ during ion exchange
Diuretics decrease clearance
Adverse FX: tremors, decrease thyroid fxn, diabetes insipidus, found in breast milk |
|
|
Term
|
Definition
Tetracyclic anti-depressent
Also for smoking cessation
lowers seizure threshold
|
|
|
Term
|
Definition
MOA:
alpha-2 antagonist = increase NE and 5HT release
5HT (2,3) antagonist
tox: sedatoin, increase appetite, wt gain, dry mouth
|
|
|
Term
|
Definition
used for Insomnia
high doeses needed for anti-depressent effects
|
|
|