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swNeurodrugs

TermDefinition
levodopa Mech /n replaces dopamine (no blood brain) converted by LAAD Pharm absorbed SI, same pump as brain Coadmin with carbidopa Adverse Effects N/V from CTZ, psychosis, dyskinesisas (5-7 yr after), arrhythimas, Ortho hypo, end of dose or on-off, comp
carbidopa Mechanism Peripheral LAAD inhibitor, allows L Dopa dosage to be lessened by 75% Pharmacokinetics Given in fixed proportion (1:4 or 1:10)
pramipexole Class dopamine receptor agonist Mechanism nonergot dopamine agonist prefer D3, high affinity for D2/D4 NO D1/D5 effect Inhibit indirect, no effect on direct Adverse nausea, somnolence, edema, hallucinations, confusion, ortho hypo, worse compul
ropinirole Class dopamine receptor agonist Mechanism nonergot dopamine agonist prefer D3, high affinity for D2/D4 NO D1/D5 effect Inhibit indirect, no effect on direct Adverse nausea, somnolence, edema, hallucinations, confusion, ortho hypo, worse compul
selegiline Class monoamine oxidase B inhibitor Mechanism selective, irreversible inhibitor of MAO-B enhances effect of LDopa, prevents end of dose and on off Adverse Effects Don't take with antidepressants, toxic effects
tolcapone Class COMT inhibitor Mechanism central/peripheral competitive inhibitor of COMT extends and increases duration of LDopa Adverse Effects Explosive diarrhea, fatal hepatotoxicity
entacapone Class COMT inhibitor Mechanism Inhibits ONLY peripheral COMT
benztropine Class Anticholinergic agents Mechanism Muscarinic antagonist Improve tremor and rigidity, not bradykinesia Adverse Effects drowsiness, delusion, moods, dry mouth, blurred vision, memory loss, dementia
diphenhydramine Class anticholinergic agents Mechanism Antihistamine Therapy Better tolerated, esp elderly Adverse Effects drowsiness, delusion, moods, dry mouth, blurred vision, memory loss, dementia
benzodiazepines Class treat spasticity Mechanism facilitate action of GABA Therapy acute muscle spasm, cerebral palsy, spinal cord lesions
baclofen Class treat spasticity Mechanism agonist of GABA-B (GPCR, hyperpolarization in spinal cord) Therapy MS, ALS, traumatic spinal cord injury Adverse Effects weakness, drowsiness, lowered seizure threshold
dantrolene Class treat spasticity Mechanism relaxes muscles by reducing Ca release from SR Therapy Malignant hyperthermia, cerebral palsy, MS Adverse Effects
Morphine Mechanism poor BBB crossing liver glucuronidated 3,6. 3 inactive, 6 more potent. mu, desc inhib of pain, hyperpol of spine and nociceptors, reducted emotional rxn Pharm Patient admin IV or strict dosing sched Adverse Effects NO in renal/liver
Codeine Mechanism medium BBB crossing Descending inhib of pain via hyperpol of PAG, RM, LC. Via mu, inhib nocicep interneurons. Reduced pain emotion Therapy Adverse Effects
Fentanyl Class Opioid Mechanism opioid. Pharmacokinetics spinal and epidural anesthesia, patch Adverse Effects
Meperidine Mechanism No miosis Therapy OB wards pain relief- shorter half life Adverse Effects toxic metabolites (no renal probs), contraindicated with MAOIs
Opioid adverse effects Euphoria, dysphoria, sedation, miosis, depression of emesis, thermoregulation (lower body temp set point, mask low fever), hyperalgesia after withdrawal, vasodilation
Oxycodone Mechanism semisynthetic opioid, codeine + NSAID
Tramadol Class Mu receptor agonist Mechanism Mu agonist, inhibits reuptake of serotonin and norephinephrine Adverse Effects Decreased seizure threshold
Diphenoxylate Class Mu agonist Mechanism minimal analgesia, used to treat diarrhea
Loperamide Class Mu agonist Mechanism minimal analgesia, used to treat diarrhea
Buprenorphine Class mixed agonist Mechanism lack full potency, less resp depression. more potent than morphine. Ceiling on effect. slow dissociation, antagonizes others Pharmacokinetics Sublingual effective, nasal for migraines
Naloxone Class Opioid antagonist Mechanism Bulky N17 group prevents activation of mu > kappa/delta. Pharmacokinetics IV or IM- NO ORAL. Short acting.
Naltrexone Class Opioid antagonist Pharmacokinetics Longer half life than Naloxone, can be given orally Therapy Block effects of injected heroine for 48 hours, reduces all other craving behavior
Pregabalin Class anticonvulsant Mechanism reduce spiking of pain neuron by inducing GABAa and inhibiting Ca (glut) Therapy Neuropathic pain AE: sedation
Gapapentin Class anticonvulsant Mechanism reduce spiking of pain neuron by inducing GABAa and inhibiting Ca (glut) Therapy Neuropathic pain (DM) Partial and generalized tonic-clonic seizure AE: sedation
phenytoin Class non sedative anti epileptic Mechanism prevents recovery of Na from inactivation Therapy partial and generalized tonic-clonic seizures Adverse Effects gingival hyperplasia, hirsutism, hepatic failure, nonlinear kinetics-toxic
carbamazepine Class Anti epileptic Mechanism Inhibits Na recovery from inactivation Therapy Simple and complex partial, tonic-clonic generalized, trigeminal neuralgia Adverse Effects Induces its own kill protein, diplopia, ataxia, aplastic anemia, agranulo
lamotrigine Class Anti epileptic Mechanism Inhibits Na recovery from inactivation Therapy Partial seizures Adverse Effects Rashes (esp pediatrics), Steven Johnson
valproic acid Class Antiepileptic Mechanism Inhibits Na recovery from inactivation Therapy Generalized myoclonic seizures, simple and complex partial, tonic-clonic generalized, absence Adverse Effects hepatotoxicity, fulminant hepatitis, teratogen- NO PREG
phenobarbital Class Anti epileptic Mechanism Enhances GABA, inhibits sodium, blocks calcium, blocks glut Therapy febrile seizures in kids, partial and generalized tonic-clonic seizures Adverse Effects toxicity, strong sedative
clonazepam Class Antiepileptic Mechanism GABA enhancer Therapy Myoclonic or absence seizures Adverse Effects drowsiness
diazepam Class benzo Mechanism GABA enhancer Therapy status epilepticus
lorazepam Class Benzo Mechanism GABA signaling enhancer Therapy status epilepticus
ethosuximide Class Anti epileptic Mechanism T type calcium inhibitor- inhibits thalamic pacemaker current, prevents rhythmic discharges. Therapy Uncomplicated absence seizures
topiramate Class Anti epileptic Mechanism Block voltage Na channels, depress glut Therapy Partial and generalized tonic-clonic seizure, migraines Adverse Effects visual problems, urolithiasis
levetiracetam Class antiepileptic Mechanism Binds synaptic vesicle protein SV2A Therapy partial, generalized tonic-clonic, and myoclonic seizures
lidocaine Class Local anesthetic Mechanism Inhibits voltage gated Na channels Amide class, use with epinephrine, medium length Therapy Most widely used agent, also anti-arrythmic Adverse Effects
mepivacaine Class local anesthetic Mechanism Inhibits voltage Na channels Use with epinephrine, medium length Adverse Effects TOXIC to neonates- NO OB
bupivacaine Class local anesthetic Mechanism inhibits voltage gated Na channels long mech of action Therapy Peripheral nerve blocks, long procedures Adverse Effects Cardiotoxicity
prilocaine Class Local anesthetic Mechanism Effective w/o vasoconstrictor, inhibits Na voltage channels, Medium action Adverse Effects Methemoglobinemia, esp in neonates- NO OB
ropivacaine Class Local anesthetic Mechanism Inhibits voltage activated Na channels, Long mech of action Adverse Effects less potent, less CV toxic, less motor block
epinephrine Class adrenergic agonist Mechanism Acts at alpha receptors, causes vasoconstriction in smooth muscle, less effective at extending lipid soluble drugs (long)
Nitrous oxide Class Anesthetic Mechanism Low blood:gas coefficient, low potency, MAC is greater than 100% Adverse Effects Can diffuse into air filled cavity super fast- NO in pneumothorax, intestinal obstruction, air embolus, trauma
Halothane Class Inhalation anesthetic Mechanism Slow induction and emergence, very potent (low MAC) Therapy Pediatric (nice smell) Adverse Effects Hepatotoxicity
Isoflurane Class Inhalation anesthetic Pharmacokinetics Very cheap, slow onset and recovery
Desflurane Class Inhalation anesthetic Pharmacokinetics Lowest b:g, rapid induction/emergence, low potency, completely eliminated through lungs Adverse Effects Airway irritation- NO in asthmatics/smokers
Sevoflurane Class Inhalation anesthetics Pharmacokinetics Slightly less rapid than des, combined with NO, pleasant smell, used in kids Adverse Effects AVOID in pts with renal toxicity
Succinylcholine Class NM blocking agent Mechanism Binds Ach receptor and promotes long depolarizations- two Ach together, not metabolized by ACHE Therapy Emergent intubation, "full stomach" Adverse Effects Bradycardia (use atropine), hyperkalemia, MH
Vecuronium and Rocuronium Class Nondepolarizing muscle relaxants Mechanism Block Ach receptors No change, no depol Therapy Routine intubation, emergent if no succ Adverse Effects reverse with cholinesterase inhibitor AND anticholinergic (brady)
Midazolam Class benzo Mechanism Enhance GABAa receptor activation Therapy Sedation/relieve anxiety, antegrade amnesia- 6 hrs, code blue b4 intubation, NO analgesia, seizures Pharm Slow onset Adverse Effects depress resp to hypercarbia, littleCV eff
Remifentanil Class Opioid Pharmacokinetics Ultra short (3 min), continuous infusion in surgery so rapid wakeup Therapy Great for neurosurgery
Thiopental Class Barbiturates Mechanism RAS, slows GABA close low, high direct stim of Cl, inhibits Ach/glut Pharmacokinetics Fast emerge, slow recovery Therapy ONLY induction in preggo Adverse Effects dec BP, inc HR, dec CBF/CMR/ICP, dec resp, neur
Etomidate Class Barbituate Mechanism Increases affinity of GABA Pharmacokinetics Rapid induction, fast emergence and medium recovery Therapy CV problems/hypotension Adverse Effects N/V, minimal cardio and resp, decrease CMR/CBF/ICP
Propofol Class Barbituate Mechanism Slows GABA closing, rapid everything Therapy Induction or maintenance, fast recovery, Amnesia no analgesia Effects less N/V, dec SVR, BP (bad in old hypo), dec CBF/CMR/ICP, apnea
Ketamine Class Barbituate Mechanism dissociates thalamus from RAS, dissociative amnesia antagonist of NMDA Pharm Rapid induct, fast recover, no apnea Therapy Sole anestheic- analgesia, amnesia, unconsciousness Adverse Effects Inc HR, CO, BP, inc
Dexmedetomidine Class Barbituates Mechanism selective a2 agonist, inhibits symp outflow/LC, substance P. Anesthesia/analgesia. Patients still breathe Pharmacokinetics Slow load neces, medium recover Adverse Effects HTN, brady if rapid, Hypo, brady if slow. A
Local anesthetic side effects sleepiness at low, convulsions/depression/death at high. vasodilation induced loss of cardiac strength and dilation of arterioles, increase resting tone of bowel smooth muscle, resp depression, ester = allergic
Adverse effects of inhalation anesthetics Decrease MAP, increase HR, decrease resp response (except NO), decrease CMR/CBF/ICP, decrease in GFR and urine output, decreased hepatic blood flow, malignant hyperthermia (minus NO)
Mech of inhalation anesthetics Decrease neuronal activity- bind ion channels directly (steep dose rsponse). Halothane binds rhodopsin. Depressed NMDA resceptors, enhance GABA receptors.
Created by: sp8cc