Pcol

Mu Receptor Agonist

Mu Receptor Agonist

• 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

• Vicodin
• Mu Receptor Agonist

• Hycodan
• Mu Receptor Agonist
• has anticholinergic effects

• 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

• Nucynta
• Mu Receptor Agonist
• Block NE re-uptake

• Oxycontin
• Mu Receptor Agonist

• Percocet
• Mu Receptor Agonist

• Percodan
• Mu Receptor Agonist

• Mu Receptor Agonist
• very long acting

• Dilaudid
• Mu Receptor Agonist
• Can cause hyperglycemia probably by reducing insulin release

Mu Receptor Agonist

Mu Receptor Agonist

• Duragesic, Actiq
• Mu Receptor Agonist

• Lomotil
• Mu Receptor Agonist peripherally

• Imodium
• Mu Receptor Agonist peripherally

Mu Receptor Agonist peripherally

Mu Receptor Agonist peripherally

• Narcan
• Mu Receptor Antagonist

Mu Receptor Antagonist

kappa agonist/ mu antagonist

kappa agonist/ mu antagonist

• Talwin
• kappa agonist/ mu antagonist

• Talwin NX
• kappa agonist/ mu antagonist

• Subutex
• Mu parital agonist/ kappa antagonist

• Suboxone
• Mu parital agonist/ kappa antagonist

• 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

• 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

• Versed
• Short acting BDZ

Pre-operative sedation, Anesthetic

• Halcion
• Short Acting BDZ

Insomnia: Fast-onset, decrease time to sleep

• Xanax
• Intermediate BDZ

Anxiety disorders, phobias, withdrawal symptoms may be severe

• Prosom
• Intermediate BDZ

Insomnia

• Ativan
• Intermediate BDZ

Anxiety disorders, IV general anesthetic, status epilepticus

• Serax
• Intermediate BDZ

Anxiety

• Restoril
• Intermediate BDZ

Insomnia

• Libirum
• Long acting BDZ

Anxiety disorders, alcohol withdrawal management, anesthetic premedication

• Klonopin
• Long acting BDZ

Seizures, adjunctive in acute mania and movement disorders. Tolerance develops to anticonvulsant activity

• Tranxene
• Long acting BDZ

Anxiety disorders, seizures

• Valium/ Diastat
• Long acting BDZ

Anxiety disorders, status epilepticus, muscle relaxants, alcohol withdrawal, anesthetic premedication

• Dalmane
• Long acting BDZ

Insomnia; active metabolites accumulate with chronic use

• Doral
• Long acting BDZ

Insomnia; active metabolites accumulate with chronic use

• 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

BDZs work as positive allosteric GABAA modulator, enhancing GABA binding affinity and/or increased channel opening frequency

• Ambien
• BDZ related

• 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

• Sonata
• BDZ like

• Lunesta
• BDZ like

• Romazicon
• BDZ antag

Binds with high affinity to GABAA to competitively antagonize the binding and allosteric effects of BDZs

BDZ OD antidote

• 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)

• Pentothal
• Ultra short acting BDZ

Anesthesia induction, short- term anesthesia maintenance, emergency seizure treatment, increased intracranial pressure

• Brevital
• ultra short Barb

Anesthesia induction, shortterm anesthesia

• Nembutal
• Ultra short Barb

Preoperative sedation, refractory status epilepticus, barbiturate coma

• Amytal
• Short acting Barb

Hypnotic, sedative

• Butisol
• Short acting barb

Anxiety, insomnia

• Fioricet, Fiorinal
• short acting barb

in combination with caffeine, acetaminophen Relief of the symptomatic complex of tension or muscle contraction headache

• Mebaral
• Short acting barb

Epilepsy, sedation

• Seconal
• Short acting barb

Sedation

• Luminal
• Long acting Barb

Anticonvulsant, status epilepticus, preoperative sedation, hypnotic

• 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

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

Buspar

selective partial agonist at the 5-HT1a receptor

• Lioresal
• GABA-b Receptor Agonist
• Centrally acting muscle relaxant

• Zanaflex
• α2 Receptor Agonists- decreases excitatory inputs to α motor neurons
• Centrally acting muscle relaxant

lower risk of hypertenion than clonidine

• Flexeril
• TCA like

• -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

• Robaxin
• Centrally acting muscle relaxant Msc

• Soma
• Centrally acting muscle relaxant Msc

• Norflex
• Centrally acting muscle relaxant Msc

• 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

• Dilantin
• seizures

• • 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

• Cerebyx
• seizures

• – Prodrug of phenytoin
• – Metabolized by plasma esterases to phenytoin
• – Similar side effects to phenytoin, less risk of hypotension

• Tegretol
• seizures

like phenytoin

• Trileptal
• Seizures

like carbamazepine

• Lamictal
• seizures

• • Na channel antagonist.
• • Binds to the inactivated conformation and slows channel recovery
• • Additional mechanism: inhibits neuronal glutamate release

• Zarontin
• seizures

• T-type Ca channel antagonist
• –Reduces the extent of Ca entry through the channel without affecting rate of recovery of channel from inactivated state

• Zonegran
• seizures

• • Inhibit T-type Ca channel through preferential binding to the inactivated state, prevents channel recovery
• • Inhibit voltage-gated Sodium channel similar to phenytoin, carbamazepine

• Neurontin
• Seizures

• Bind specific α2 δ subunit of voltage-gated calcium channel, reduces Ca influx mediated neurotransmitter release (Glu, NE, DA, substance P)

• Lyrica
• Seizures

Bind specific α2 δ subunit of voltage-gated calcium channel, reduces Ca influx mediated neurotransmitter release (Glu, NE, DA, substance P)

• Gabitril
• Seizures

Inhibits GAT-1 transporter

• Sabril
• Seizures

Irreversible inhibitor of GABA-T

• Depakote
• Seizures

• • Na channel antagonist (similar mechanism to phenytoin)
• • T-type Ca channel antagonist
• • Enhancing GABA transmission via increase in GABA neuronal content

• Keppra
• Seizures

• • Inhibition of High-voltage gated Ca channels
• • Inhibition of excitatory neurotransmitter release
• •Reversal of zinc-induced inhibition of GABAA receptors

Topamax

• AMPA Receptor: Ligand-gated Na channel
• AMPA Receptor antagonist: Topiramate

• 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

• NMDA Receptor: Ligand-gated Ca channel
• –NMDA Receptor antagonist

Inhalation anesthetics

Inhalation anesthetics

Inhalation anesthetics

Inhalation anesthetics

Inhalation anesthetics

Inhalation anesthetics

NMDA receptor antagonist effect

IV anesthetics

• Diprivan
• IV anesthetics

• –Targets GABA-A receptors
• –Voltage-gated Na+channel antagonist

• Amidate
• IV anesthetics

-Agonist at GABAAreceptor

– Inhibits glucocorticoid and mineralocorticoid synthesis

• Ketalar
• IV anesthetics

• – NMDA Noncompetitive Receptor Antagonist
• – α1and β1receptor agonist
• – Prevents re-uptake of catecholamines

causes emergence phenomenon

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

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

• antidote for malignant hyperthermia
• Direct acting muscle relaxant

Inhibits release of Ca2+ release from sarcoplasmic reticulum by binding to ryanodine receptor

• –Triptans
• –Ergots
• –NSAIDs, aspirin, acetaminophen (Treximet= sumatriptan+ naproxen)
• –Fiorinalor Fioricet (Aspirin or acetaminophen, plus butalbital plus caffeine)
• –Opiates

• –propranolol
• –verapamil
• –divalproex, topiramate
• –ACE inhibitors, ARBs
• –botulinumtoxin type A (Botox)

• Imitrex
• triptans- migraines

• Axert
• triptans- migraines

• Zomig
• triptans- migraines

• Amerge
• triptans- migraines

• Maxalt
• triptans- migraines

• Frova
• triptans- migraines

• Relpax
• triptans- migraines

ergots- migraines

ergots- migraines

• methylergonovine
• ergots- migraines

ergots- migraines

Indirect-acting sympathomimetics, Amphetamines

• dextroamphetamine
• Indirect-acting sympathomimetics, Amphetamines

• methamphetamine
• Indirect-acting sympathomimetics, Amphetamines

• lisdexamfetamine
• Indirect-acting sympathomimetics, Amphetamines

Indirect-acting sympathomimetics, Methylphenidates

Indirect-acting sympathomimetics, Methylphenidates

• dexmethylphenidate
• Indirect-acting sympathomimetics, Methylphenidate

• Didrex
• Indirect-acting sympathomimetics, msc

Indirect-acting sympathomimetics, msc

Indirect-acting sympathomimetics, msc

• Fen-phen
• Indirect-acting sympathomimetics, msc

• Meridia
• Indirect-acting sympathomimetics, msc

• Provigil
• Indirect-acting sympathomimetics, msc

• Nuvigil
• Indirect-acting sympathomimetics, msc

Indirect-acting sympathomimetics, msc

• Strattera
• Indirect-acting sympathomimetics, msc

• TCA
• antidepressants

• TCA
• antidepressants

• TCA
• antidepressants

• Elavil
• TCA
• antidepressants

• TCA
• antidepressants

• TCA
• antidepressants

• TCA
• antidepressants

• TCA
• antidepressants

• TCA
• antidepressants

• TCA
• antidepressants

SSRI antidepressants

• Zoloft
• SSRI antidepressants

• Celexa
• SSRI antidepressants

• Paxil
• SSRI antidepressants

• Lexapro
• SSRI antidepressants

• Prozac
• SSRI antidepressants

• Effexor
• SNRI antidepressants

• Pristiq
• SNRI antidepressants

• Cymbalta
• SNRI antidepressants

• Savella
• SNRI antidepressants

• Nardil
• MAOi antidepressants

MAOi antidepressants

• Wellbutrin
• Atypical antidepressants

Atypical antidepressants

Atypical antidepressants

Atypical antidepressants

Bi-polar