8-24 Muscle Relaxers/Serotonin/Dopamine/Opiods/ Anesthetics Flashcards
Baclofen:
Mechanism of Action
GABA agonist
Inhibits neurotransmitter
release from skeletal muscle sensory afferent- (by inhibiting calcium influx and therefore reducing the release of excitatory transmitters)
Baclofen:
Rx
ΒΊmuscle spasticity assoc.
with multiple sclerosis or Spinal Cord Injury
Baclofen:
Side Effects (1)
Drowsiness
Diazepam:
Mechanism of Action
Benzodiazepine receptor agonist
Diazepam:
Rx (2):
- Muscle spasm due to local injury (inflammation),
2. muscle spasticity due to loss of descending inhibitory input, (e.g.cerebral palsy)
General for benzodiazepines
(Diazepam, cloneazepamβ¦)
Mechanism of Action (1):
Facilitate GABA mediated pre-synaptic inhibition
General for benzodiazepines
(Diazepam, cloneazepamβ¦)
Clinical usages (2)
- Spinal Spasticity
2. Multiple Sclerosis
General for benzodiazepines
(Diazepam, cloneazepamβ¦)
Side effects (2)
Sedation
Drowsiness
Rocuronium
Duration of Action
25 mins
Rocuronium
MOA
[Non-Depolarizing Muscular Nicotinic BLOCKER]
Rocuronium
Location of Elimination
Liver
Rocuronium
Rx (2)
- Intubation
2. Muscle relaxation during surgery or ventilation
Mivacurium
Duration of Action
15-20min
Mivacurium
MOA
[Non-Depolarizing Muscular Nicotinic BLOCKER]
Mivacurium
Elimination
Plasma cholinesterase
Mivacurium
Rx. (2)
- Intubation
2. Muscle relaxation during surgery or ventilation in pts w/ renal failure
Vecuronium
Duration of action
30-45 min
Vecuronium
MOA
[Non-Depolarizing Muscular Nicotinic BLOCKER]
Vecuronium
Elmination (2)
- Liver (metabolism and clearance)
2. Renal (elimination)
Vecuronium
Rx (2)
Adjuvant in Surgical Anesthesia for:
1) Abdominal Wall Relaxation
2) Orthopedic Procedures
Bromocriptine
Mechanism of Action
D2 Agonist
Bromocriptine
Rx
Parkinsonβs Disease
Carbidopa
Mechanism of Action
Aromatic acid decarboxylase inhibitor
Carbidopa
Rx
Parkinsonβs Disease
Carbidopa
Side Effects (2)
Same as L-Dopa since it increases L-Dopa β> arrhythmia, dyskinesia
Selegiline
Mechanism of Action
MAO-b inhibitor
Selegiline
Rx
Parkinsonβs disease
Talcapone
Mechanism of Action
COMT inhibitor
Talcapone
Rx
Parkinsonβs disease
Methylphenidate
Mechanism of Action
Dopamine reuptake inhibitor
Methylphenidate
Rx
ADHD
Methylphenidate
Side effect
Tachycardia
Mu (OP3)
Locations (6)
Brain:
- cortex (lamina III-IV)
- Thalamus
- Striosomes
- periaqueductal gray
Spinal Cord
- substantial gelatinosa
-Intestinal tract
Mu - subtype 1
Function (2)
- Supraspinal analgesia
- physical dependence
Mu - subtype 2
Function (5)
- Respiratory depression
- miosis
- euphoria
- reduced GI mobility
- physical dependence
β Mu2 was a kinda GRUMP β
Mu - subtype 3
Function
unknown
Naloxone
Receptors - antagonist/agonist (3)
mu-R: antagonist
Delta-R: antagonist
Kappa-R:antagonist
Naloxone
A: Used for:
B: Its indication helps prevent/reduce effects such asβ¦(3)
C: Has NO _______ properties characteristic of other narcotic antagonist
Naloxone
A: antidote for opioid overdose
B: prevents or reverses effects of opioids including respiratory depression, sedation and hypotension
C: NO [agonistic or morphine-like] properties characteristics of other narcotic antagonist
Naloxone
Side Effects (4)
- Change in mood
- Trembling
- Change in heart rhythm
- Block the action of pain-lowering endorphins
MethaDone
Receptor - Antagonist/agonist (2)
mu - agonist
delta- agonist
- (M)etha(D)one *
MethaDone
Side effects
Firm occupancy of opioid receptors by MethaDone ____ (INC/DEC) desire for other opioid intake, because it is producing a _______ but ___ (INC/DEC) effect which attenuates withdrawal manifestations.
dependence
Firm occupancy of opioid receptors by MethaDone DEC desire for other opioid intake, because it is producing a LONGER but DEC EFFECT which attenuates withdrawal manifestations.
MethaDone
Function
Treats Opioid Dependence
Tizanidine
Physiological effect:
[CENTRAL a2 agonist] that acts on pre and post-synpatic nerves of Spinal Cord β> Inhibition
Tizanidine
Indication (2)
Multiple sclerosis
Spinal spasticity
Tizanidine
Toxicity (2)
Drowsiness
Hypotension
Dantrolene
Physiological Actions
Blocks calcium release from SR of skeletal muscle
Dantrolene
Indications (5)
- SPASMS 2ΒΊ to Stroke
- SPASMS 2ΒΊ to Spinal Cord Injury
- Malignant Hyperthermia
- Cerebral Palsy
- Multiple Sclerosis
Dantrolene
Toxicity (3)
- Muscle weakness
- Sedation
- Hepatitis
Metaclopramide
MOA:
Side effects (2) :
MOA: [D2 Blocker] with some [5HT4 agonist]
SE: [Focal dystonia], Akathisia, [Tardive Dystonia after 3 months]
M.SE.FAT
Metaclopramide:
Contraindications:
Contraindications: long-term rx (3 months
can cause tardive dyskinesia)
Haloperidol
MOA:
Indications (2):
MOA: [D2 Blocker]
Indications:
ΒΊacute psychosis
ΒΊlong-term depot for poorly compliant schizophrenic
patients
Haloperidol
Side Effects:
extrapyramidal motor disturbances
Trazadone MOA (2)
[5-HT2A/2C BLOCKER] + SSRI
Trazadone Indications (2)
Anxiety/depression
Trazadone
SE
Warning of suicidality in young adults at initiation of treatment
Trazadone
Contraindicaitons
MAO inhibitors
Nociceptin receptor
(OP4)
Subtypes
ORL1
Nociceptin receptor location (7)
Brain:
- Cortex
- Amygdala
- hippocampus
- septal nuclei
- habenula
- hypothalamus
Spinal cord
Nociceptin function (3)
- anxiety
- depression
- appetite
Pentazocin
Receptor subtypes and action
m-receptor: antagonist
d-receptor: agonist
K-receptor: agonist
Pentazocin
Indications
Dental extraction
Pantazocin
Side Effects: (2)
- Hallucinations/Psychomimetic Effects
2. Cardiovascular effects
5-HTP
Mechanism of Action
5-HT Precursor
5-HTP
Rx
Depression
Buspirone
Mechanism of Action
5-HT1A partial agonist
Buspirone
Rx (2)
Anxiety/depression
Buspirone
Side Effects
Early increase in anxiety
Sumatriptan
Mechanism of Action
5-HT1D agonist
Sumatriptan
Rx
Migraine
Sumatriptan
Side Effects
Coronary vasoconstriction
Risperidone
Mechanism of Action
5-HT2A/2C BLOCKER
Risperidone
Rx (2)
- Depression
- Psychosis
Risperidone
Side Effects (2)
- Akathisia (also occurs as Metaclopramide SE)
2. Weight Gain
Odansetron
Mechanism of Action
5-HT3
Odansetron
Rx
Chemotherapy-induced emisis
Fluoxetine
Mechanism of Action
SSRI
Fluoxetine
Rx (6)
- OCD
- Depression
- Anxiety
- Panic Disorder
- PTSD
- Social Phobia
β Youβll need SSRIβs if you [OD on APPS] β
Fluoxetine
Side Effects (2)
Sexual Dysfunction
Insomnia
Sertraline
Mechanism of Action
SSRI
Sertraline
Rx (6)
- OCD
- Depression
- Anxiety
- Panic Disorder
- PTSD
- Social Phobia
β Youβll need SSRIβs if you [OD on APPS] β
Sertraline
Side Effects (2)
Sexual Dysfunction
Insomnia
L-DOPA
Mechanism of Action
Dopamine Precursor
L-DOPA
Rx
Parkinsonβs Disease
L-DOPA
Side Effects (2)
Arrythmia
Dyskinesia
Delta (OP1)
Subtypes (2)
Delta 1
Delta 2
Delta (OP1)
Location (4)
Brain
- Pontine Nuclei
- Amygdala
- Olfactory bulbs
- Deep Cortex
Delta (OP1)
Function (3)
- Analgesia
- Antidepressant effects
- Physical dependence
Kappa (OP2)
Subtypes (3)
Kappa 1
Kappa 2
Kappa 3
Kappa (OP2)
Location (4)
Brain:
- Hypothalamus
- Periaqueductal Gray
- Claustrum
Spinal Cord:
-Substantia Gelatinosa
Kappa (OP2)
Function (5)
- Miosis (and MEPERIDINE uses this receptor)
- Inhibits ADH release
- Sedation
- Spinal Analgesia
-Dysphoria
β [MISS D] loved her some Kappasβ
Morphine
receptor type
Mu
Morphine
Indication
severe pain
Morphine
Side Effects (3)
(x) Constipation
(x) Addiction
(x) Tolerance
Morphine
Antidote
Naloxone
Meperidine
Receptor type
Kappa receptor
Meperidine
Indication
Severe pain
Meperidine
Side Effects (4)
- Seizure
- Dysphoria
- Tremor
- Respiratory Depression
Meperidine
Other Notes (2)
1) Also binds: K+ channels, Muscarinic receptors, Dopamine transporter
2) Do not use Naloxone as andtidote
Hydrocodone
Receptor types (2)
Mu
Delta
Hydrocodone
Indication (2)
- Moderate pain
2. Coughing (anti-tussive)
Hydrocodone
Side Effects (3)
- Constipation
- Respiratory Depression
- Nausea
Hydrocodone
Other note
Recreational Drug
Codeine
Receptor type
Mu receptor
Codeine (4)
Indications
- Irritable Bowel Syndrome
- Narcolepsy
- Diarrhea
- Cough
βWhy would I need Codeine [IN DC] ? β
Codeine
Side Effects (5)
- Euphoria
- Itching
- Urinary Retention
- Depression
- Constipation
Codeine
Other Note
Active metabolite is morphine
Procaine (HCl)
Potency
1
Procaine (HCl)
Onset of Analgesia
Slow
Procaine (HCl)
Duration of Action
Short (30 - 45 min)
Procaine (HCl)
Anesthetic Use
Infiltrative Nerve Block: Subarachnoid
Cocaine (HCl)
Potency
2
Cocaine (HCl)
Onset of Analgesia
Rapid (1 min)
Cocaine (HCl)
Duration of Action
Medium (1 hr)
Cocaine (HCl)
Anesthetic Use
Topical
Easily absorbed through mucous membrane
Tetracaine (HCl)
Potency
16
Tetracaine (HCl)
Onset of Analgesia
Slow for Spinal (15 - 20 min)
Tetracaine (HCl)
Duration of Action
Long (2-5 hr)
Tetracaine (HCl)
Anesthetic Use
Subarachnoid
Benzocaine
Potency
(Topical use only)
poorly water soluble
dusting powder/ointment for wounds without concerns for systemic toxicity
Benzocaine
Onset of Analgesia
Dependent upon pharmaceutical formulation
Benzocaine
Duration of Action
Dependent upon pharmaceutical formulation
Benzocaine
Anesthetic Use
Topical
Lidocaine (HCl)
(Xylocaine)
Potency
4
Lidocaine (HCl)
(Xylocaine)
Onset of Analgesic
Rapid
Lidocaine (HCl)
(Xylocaine)
Duration of Action
Medium (1.25 hr)
Lidocaine (HCl)
(Xylocaine)
Anesthetic Use (4 Locations of Administration)
Infiltrative Nerve Block: Intravenous- Epidural Subarachnoid Regional
Mepivacaine (HCl)
(Carbocaine)
Potency
2
Mepivacaine (HCl)
(Carbocaine)
Onset of Analgesia
Rapid (3-5 min)
Mepivacaine (HCl)
(Carbocaine)
Duration of Action
Medium
Mepivacaine (HCl)
(Carbocaine)
Anesthetic Use (2)
Infiltrative Nerve Block:
Epidural
Ketamine
MOA
[NMDA RECEPTOR BLOCKER]
Ketamine
Description of anesthesia
Dissociative anesthesia
Ketamine
Physiological effects (6)
INCREASES in:
- CMR O2 (Cerebral Metabolic Rate)
- HR
- Intra Cranial Pressure (ICP)
- Cerebral Blood Flow
- BP
- BronchoDilation
β Ketamine INC that [C.H.I.C. BP] β
A: List the 4 Systemic Effects of Propofol?
B: How is Propofol administered?
A:
1) DEC Intracranial Pressure
2) DEC CMRO2 of the brain
3) Vaso/venoDILATES β> Reduces both preload AND Afterload
4) Respiratory Depression
B: Propofol Route of Administration: INTRAVENOUS
A: Ketamine is very strongly used as a ___Dilator
B: What does it do to these factors?
- CMRO2
- Cerebral blood flow
- Intracranial Pressure
- Blood Pressure
- HR
C: MOA for Ketamine?
D: What are its 2 indications?
A: Ketamine is very strongly used as a BRONCHODILATOR
B: What does it do to these factors?
- CMRO2 = INC
- Cerebral blood flow = INC
- Intracranial Pressure = INC
- Blood Pressure = INC
- HR = INC
C: MOA for Ketamine?
[NMDA Receptor BLOCKER]
D: ΒΊShort Procedures ΒΊAnesthetic Inducer
3 Side Effects of Ketamine
1) Bad Dreams
2) Salivation
3) Twitching
A: Whatβs the most dangerous side effect of [Intravenous Thiopental]?
B: Does Thiopental INC or DEC CMRO2?
A: Thiopental is a vasoCONSTRICTOR β> LIMB ISCHEMIA!
B: Thiopental still DEC CMRO2 in the brain
A: Which IV Anesthetic has the least cardiovascular side effects?
B: What is the primary SIDE EFFECT for this [IV Anesthetic]?
C: This [IV Anesthetic] is a _______ [vasoDilator/vasoCONSTRICTOR] and will ______[INC/DEC] CMRO2
A: ETOMIDATE
B: Adrenal Suppression: Pt will not produce [Adrenal NorEpi] and thus be UNABLE TO MAINTAIN THEIR OWN BP
C: This [IV Anesthetic] is a vasoconstrictor and will DEC CMRO2 {like Thiopental}
Pancuronium
Duration of Action
30 - 60 min
Pancuronium
Mechanism of Action
Non-depolarizing blockade of muscle
Nicotinic receptors
Pancuronium
Elimination
Primarily renal excretion
Pancuronium
Rx (2)
Adjuvant in Surgical Anesthesia for:
1) Abdominal Wall Relaxation
2) Orthopedic Procedures
(same as Vecuronium)
D-Tubocurarine
Duration of Action
> 60 min
D-Tubocurarine
Mechanism of Action
[Non-Depolarizing Muscular Nicotinic Blocker]
D-Tubocurarine
Elimination
Liver clearance and renal elimination
D-Tubocurarine
Rx
Prototype
only used in lethal injection