-
Morphine
Mu Receptor Agonist
-
Codeine
Mu Receptor Agonist
-
Meperidine
- Demerol
- Mu Receptor Agonist
- There is a metabolite called normeperidine
- Normeperidine has a long half-life, and can cause seizures
- Because this metabolite builds up, meperidine should not be used for more than 48 hours
-
Hydrocodone w/ APAP
- Vicodin
- Mu Receptor Agonist
-
Hydrocodone w homatropine
- Hycodan
- Mu Receptor Agonist
- has anticholinergic effects
-
Tramadol
- Ultram
- Mu Receptor Agonist
- Can inhibit the reuptake of NE and 5-HT
- Reduces levels of substance P and glutamate
- may also be able to directly activate alpha-2 receptors, creating an analgesic effect
-
Tapentadol
- Nucynta
- Mu Receptor Agonist
- Block NE re-uptake
-
Oxycodone CR
- Oxycontin
- Mu Receptor Agonist
-
Oxycondone w/ APAP
- Percocet
- Mu Receptor Agonist
-
Oxycodone w/ASA
- Percodan
- Mu Receptor Agonist
-
Methadone
- Mu Receptor Agonist
- very long acting
-
Hydromorphone
- Dilaudid
- Mu Receptor Agonist
- Can cause hyperglycemia probably by reducing insulin release
-
Oxymorphone
Mu Receptor Agonist
-
Levorphanol
Mu Receptor Agonist
-
Fentanyl
- Duragesic, Actiq
- Mu Receptor Agonist
-
Diphenoxylate w/ atropine
- Lomotil
- Mu Receptor Agonist peripherally
-
Loperamide
- Imodium
- Mu Receptor Agonist peripherally
-
Paregoric
Mu Receptor Agonist peripherally
-
DTO (deodorized tincture of opium)
Mu Receptor Agonist peripherally
-
Naloxone
- Narcan
- Mu Receptor Antagonist
-
Naltrexone
Mu Receptor Antagonist
-
Nalbuphine
kappa agonist/ mu antagonist
-
Butorphanol
kappa agonist/ mu antagonist
-
Pentazocine
- Talwin
- kappa agonist/ mu antagonist
-
Pentazocine and Naloxone
- Talwin NX
- kappa agonist/ mu antagonist
-
Buprenorphine
- Subutex
- Mu parital agonist/ kappa antagonist
-
Buprenorphine w. naloxone
- Suboxone
- Mu parital agonist/ kappa antagonist
-
Ziconotide
- Prialt
- Conotoxin
- block N type calcium channels-Keep it more likely in the closed state
- Ca cant enter channels, less NT released, Fewer impulses and less perception of pain(activation of the Mu receptors in dorsal horn decreases the release of NT) --> reducing activation of ascendingneuron
- intrathecal injection Bc that is where the effect is
- Doesn’t reach MOR in the brain (No respiratory depression, No euphoria.
- Blocking these Ca channels give significant analgesia without the side effects fromactivating the Mu receptors in the brain
-
BDZ therapeutic use
- Anxiolytics
- Treatment of insomnia
- Treatment of alcohol withdrawal syndrome
- Anticonvulsants: Agents with rapid onset of action is used in treatment of status epilepticus. Chronic treatment is associated with development of tolerance
- Muscle relaxants: Reduce skeletal muscle spasticity by enhancing the activity of inhibitory neurotransmission in the spinal cord
-
Midazolam
Pre-operative sedation, Anesthetic
-
Triazolam
Insomnia: Fast-onset, decrease time to sleep
-
Alpazolam
Anxiety disorders, phobias, withdrawal symptoms may be severe
-
-
Lorazepam
Anxiety disorders, IV general anesthetic, status epilepticus
-
-
-
Chlordiazepoxide
Anxiety disorders, alcohol withdrawal management, anesthetic premedication
-
Clonazepam
Seizures, adjunctive in acute mania and movement disorders. Tolerance develops to anticonvulsant activity
-
Clorazepate
Anxiety disorders, seizures
-
Diazepam
- Valium/ Diastat
- Long acting BDZ
Anxiety disorders, status epilepticus, muscle relaxants, alcohol withdrawal, anesthetic premedication
-
Flurazepam
Insomnia; active metabolites accumulate with chronic use
-
Quazepam
Insomnia; active metabolites accumulate with chronic use
-
BDZ side effects
- Lightheadedness, mental impairment, loss of motor function coordination, confusion, anterograde amnesia (additive effect with alcohol, other sedative/hypnotic drugs)
- Paradoxical effects: anxiety, irritability, tachycardia, sweating, hallucinations
-
BDZ mech of action
BDZs work as positive allosteric GABAA modulator, enhancing GABA binding affinity and/or increased channel opening frequency
-
-
BDZ like drugs mech of action
- Selective for α1GABAA. Binds to the same site as
- Used in treatment of insomnia –Lack anticonvulsant, anxiolytic or
- muscle-relaxant effects of BDZs
- Side-effects: Amnesia, impairment of complex task performance similar to BDZs, may have similar abuse potential
-
-
-
Flumazenil
Binds with high affinity to GABAA to competitively antagonize the binding and allosteric effects of BDZs
BDZ OD antidote
-
Barbiturates Mech of Action
- Like BDZs, a positive GABAA allosteric receptor modulator increasing Cl- current
- Site of binding to GABAA receptor is distinct from GABA and BDZs
- Weak agonist activity at GABAA receptor (Direct opening of Cl- channel)
-
Thiopental
- Pentothal
- Ultra short acting BDZ
Anesthesia induction, short- term anesthesia maintenance, emergency seizure treatment, increased intracranial pressure
-
Methohexital
Anesthesia induction, shortterm anesthesia
-
Pentobrabital
Preoperative sedation, refractory status epilepticus, barbiturate coma
-
-
-
Butalbital
- Fioricet, Fiorinal
- short acting barb
in combination with caffeine, acetaminophen Relief of the symptomatic complex of tension or muscle contraction headache
-
-
-
Phenobarbital
Anticonvulsant, status epilepticus, preoperative sedation, hypnotic
-
Barb Side effects
- CNS depression, additive effects with other CNS depressants, e.g. BZDs and ethanol
- Respiration: Depress respiratory drive and mechanisms for rhythmic control of respiration
- Impaired motor skills, drowsiness
- Generally, no significant effect on hemodynamics. In overdoses, blood pressure lowering and cardiac arrhythmia
- Paradoxical excitement
-
Ramelteon
Rozerem
- -MT1 and MT2 receptor agonist
- -MT1 and MT2 are present within the suprachiasmic nucleus of the hypothalamus
- Endogenous agonist is melatonin
- -MT1 activation induces sleep, MT2 activation regulates circadian rhythm
- -Ramelteon is more selective for MT1 compared to MT2
-
Buspirone
Buspar
selective partial agonist at the 5-HT1a receptor
-
Baclofen
- Lioresal
- GABA-b Receptor Agonist
- Centrally acting muscle relaxant
-
Tizanidine
Clonidine
- Zanaflex
- α2 Receptor Agonists- decreases excitatory inputs to α motor neurons
- Centrally acting muscle relaxant
lower risk of hypertenion than clonidine
-
Cyclobenzaprine
- -inhibits NET
- -anticholingeric effects
- -5-HT2 receptor antagonist at the spinal level
- -Alpha motor neuronal activity is regulated by descending serotonergic neurons from medullary raphe
-
Methocarbamol
- Robaxin
- Centrally acting muscle relaxant Msc
-
Carisoprodol
- Soma
- Centrally acting muscle relaxant Msc
-
Orphenadrine
- Norflex
- Centrally acting muscle relaxant Msc
-
Gaba-b receptors
- Metabotropic receptor (GPCR): Heterodimers composed of R1 and R2 subunits.
- Endogenous agonist: GABA • Present pre-synaptically and post-synaptically
- Pre-synapse: Inhibition of Ca2+ entry
- Post-synapse: Stimulation of K+ efflux
-
Phenytoin
- • Binds to voltage-gated Na+ channel in the inactivated state
- • Slows recovery of Na channel to the closed conformation
- • Use-dependent channel antagonism
- • non linear kinetics
-
Fosphenytoin
- – Prodrug of phenytoin
- – Metabolized by plasma esterases to phenytoin
- – Similar side effects to phenytoin, less risk of hypotension
-
-
-
Lamotrigine
- • Na channel antagonist.
- • Binds to the inactivated conformation and slows channel recovery
- • Additional mechanism: inhibits neuronal glutamate release
-
Ethosuximide
- T-type Ca channel antagonist
- –Reduces the extent of Ca entry through the channel without affecting rate of recovery of channel from inactivated state
-
Zonisamide
- • Inhibit T-type Ca channel through preferential binding to the inactivated state, prevents channel recovery
- • Inhibit voltage-gated Sodium channel similar to phenytoin, carbamazepine
-
Gabapentin
- Bind specific α2 δ subunit of voltage-gated calcium channel, reduces Ca influx mediated neurotransmitter release (Glu, NE, DA, substance P)
-
Pregabalin
Bind specific α2 δ subunit of voltage-gated calcium channel, reduces Ca influx mediated neurotransmitter release (Glu, NE, DA, substance P)
-
Tiagabine
Inhibits GAT-1 transporter
-
Vigabatrin
Irreversible inhibitor of GABA-T
-
Valproic Acid
- • Na channel antagonist (similar mechanism to phenytoin)
- • T-type Ca channel antagonist
- • Enhancing GABA transmission via increase in GABA neuronal content
-
Levetiracetam
- • Inhibition of High-voltage gated Ca channels
- • Inhibition of excitatory neurotransmitter release
- •Reversal of zinc-induced inhibition of GABAA receptors
-
Topiramate
Topamax
- AMPA Receptor: Ligand-gated Na channel
- AMPA Receptor antagonist: Topiramate
-
Inhalation anesthetics MOA
- Not clearly identified
- Highly lipophilic
- Thought to exert non-specific effect on plasma membrane of excitable neurons leading to stabilization of hyperpolarized state
- GABAAstimulation and K+channel agonists
-
Felbamate
- NMDA Receptor: Ligand-gated Ca channel
- –NMDA Receptor antagonist
-
Isoflurane
Inhalation anesthetics
-
Enflurane
Inhalation anesthetics
-
Desflurane
Inhalation anesthetics
-
Sevoflurane
Inhalation anesthetics
-
Halothane
Inhalation anesthetics
-
Nitrous Oxide
Inhalation anesthetics
NMDA receptor antagonist effect
-
Thiopental
IV anesthetics
-
Propofol
- –Targets GABA-A receptors
- –Voltage-gated Na+channel antagonist
-
Etomidate
-Agonist at GABAAreceptor
– Inhibits glucocorticoid and mineralocorticoid synthesis
-
Ketamine
- – NMDA Noncompetitive Receptor Antagonist
- – α1and β1receptor agonist
- – Prevents re-uptake of catecholamines
causes emergence phenomenon
-
MinimumAlveolarConcentratio
Inhalational anesthetic %volume of inspired air at which 50% of patients do not respond to a surgical stimulus
The lower the MAC, the higher the potency
-
Malignant Hyperthermia
Rare complication of inhalational general anesthetics, and depolarizing neuromuscular blockers
- Increase cytoplasmic free Calcium in skeletal muscle cells (Rigidity, spasms)
- – Increase body temperature
- – Hypermetabolism: Increase oxygen consumption and CO2 production
- – Muscle cell damage, sympathetic activation
-
Dantrolene
- antidote for malignant hyperthermia
- Direct acting muscle relaxant
Inhibits release of Ca2+ release from sarcoplasmic reticulum by binding to ryanodine receptor
-
Abortive treatments for migraines
- –Triptans
- –Ergots
- –NSAIDs, aspirin, acetaminophen (Treximet= sumatriptan+ naproxen)
- –Fiorinalor Fioricet (Aspirin or acetaminophen, plus butalbital plus caffeine)
- –Opiates
-
Preventive treatments for migraines
- –propranolol
- –verapamil
- –divalproex, topiramate
- –ACE inhibitors, ARBs
- –botulinumtoxin type A (Botox)
-
Sumatriptan
- Imitrextriptans- migraines
-
-
-
Naratriptan
- Amerge
- triptans- migraines
-
Rizatriptan
- Maxalt
- triptans- migraines
-
-
Eletriptan
- Relpaxtriptans- migraines
-
Ergotamine
ergots- migraines
-
Dihydroergotamine
ergots- migraines
-
Methergine
- methylergonovine
- ergots- migraines
-
Bromocriptine
ergots- migraines
-
Adderall
Indirect-acting sympathomimetics, Amphetamines
-
Dexedrine
- dextroamphetamine
- Indirect-acting sympathomimetics, Amphetamines
-
Desoxyn
- methamphetamine
- Indirect-acting sympathomimetics, Amphetamines
-
Vyvanse
- lisdexamfetamine
- Indirect-acting sympathomimetics, Amphetamines
-
Ritalin
Indirect-acting sympathomimetics, Methylphenidates
-
Concerta
Indirect-acting sympathomimetics, Methylphenidates
-
Focalin
- dexmethylphenidate
- Indirect-acting sympathomimetics, Methylphenidate
-
Benzphetamine
- Didrex
- Indirect-acting sympathomimetics, msc
-
Diethylpropion
Indirect-acting sympathomimetics, msc
-
Phendimetrazine
Indirect-acting sympathomimetics, msc
-
fenfluramine(or dexfenfluramine) plus phentermine
- Fen-phen
- Indirect-acting sympathomimetics, msc
-
Sibutramine
- Meridia
- Indirect-acting sympathomimetics, msc
-
Modafinil
- Provigil
- Indirect-acting sympathomimetics, msc
-
Armadafinil
- Nuvigil
- Indirect-acting sympathomimetics, msc
-
ephedrine
Indirect-acting sympathomimetics, msc
-
Atomoxitene
- Strattera
- Indirect-acting sympathomimetics, msc
-
-
-
-
-
-
-
-
-
-
-
Fluvoxamine
SSRI antidepressants
-
Sertraline
- Zoloft
- SSRI antidepressants
-
Citalopram
- Celexa
- SSRI antidepressants
-
Paroxetine
- Paxil
- SSRI antidepressants
-
Escitalopram
- Lexapro
- SSRI antidepressants
-
Fluoxetine
- Prozac
- SSRI antidepressants
-
Venlafaxine
- Effexor
- SNRI antidepressants
-
Desvenlafaxine
- Pristiq
- SNRI antidepressants
-
Duloxetine
- Cymbalta
- SNRI antidepressants
-
Milnacipran
- Savella
- SNRI antidepressants
-
Phenelzine
- Nardil
- MAOi antidepressants
-
Tranylcypromine
MAOi antidepressants
-
Bupropion
- Wellbutrin
- Atypical antidepressants
-
Mirtazapine
Atypical antidepressants
-
Nefazodone
Atypical antidepressants
-
Trazodone
Atypical antidepressants
-
|
|