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swNeurodrugs
Term | Definition |
---|---|
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. |