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460 Cards in this Set
- Front
- Back
|
Symptoms used to diagnose opiate overdose
|
Respiratory Depression
Pinpoint pupils CNS depression |
|
|
Possible therapeutic effects of Opioids
|
Analgesic
Antitussive Antidiarrheal |
|
|
Effects of activation of MOR receptors in the CNS
|
Analgesia
Euphoria CNS Depression Respiratory Depression Miosis Low Seizure Threshold Nausea Vomiting Antitussive |
|
|
Stimulation of kappa opioid receptors is not related to drug abuse because
|
Dysphoria causes a sense of doom
|
|
|
Peripheral effects of MOR activation
|
Constipation
Urgency Hesitancy Histamine Release Decrease immune function long term |
|
|
Cardiac surgery is contraindicated with opioids peripheral effects:
|
Histamine release causes vasodilation leading to reflex tachychardia
|
|
|
morphine
|
Mu receptor agonist
|
|
|
codeine
|
Mu receptor agonist
|
|
|
meperidine (Demerol)
|
Mu receptor agonist
|
|
|
hydrocodone
w/ APAP = Vicodin |
Mu receptor agonist
|
|
|
hydrocodone
w/ homatropine = Hycodan |
Mu receptor agonist
|
|
|
tramadol (Ultram)
|
Mu receptor agonist
|
|
|
tapentadol (Nucynta)
|
Mu receptor agonist
|
|
|
oxycodone
Controlled release = Oxycontin |
Mu receptor agonist
|
|
|
oxycodone
w/ APAP = Percocet |
Mu receptor agonist
|
|
|
oxycodone
w/ ASA = Percodan |
Mu receptor agonist
|
|
|
methadone
|
Mu Receptor Agonist
|
|
|
hydromorphone (Dilaudid)
|
Mu Receptor Agonist
|
|
|
oxymorphone
|
Mu Receptor Agonist
|
|
|
levorphanol
|
Mu Receptor Agonist
|
|
|
fentanyl (Duragesic, Actiq)
|
Mu Receptor Agonist
|
|
|
Pharmacogenomic consideration for codeine
|
Low 2D6 activity decreases analgesic effect
|
|
|
Meperidine should only be used acutely <48hr because
|
very likely to cause seizures
|
|
|
After phase 2 metabolism of morphine, its metabolite _________ gets into the brain and is more potent
|
morphine-6-glucuronide
|
|
|
tramadol can inhibit the reuptake of ____ and ____
|
norepinephrine
serotonin |
|
|
methadone is used to help treat opioid addiction because of its ________ properties
|
methadone is less lipophilic and longer acting to provide analgesia without rush euphoria
|
|
|
hydromorphone can cause _____glycemia
|
hyperglycemia
|
|
|
This is the most potent mu agonist; often used transdermally
|
sufentanyl
|
|
|
Diphenoxylate
|
Peripheral Mu Agonist
|
|
|
Diphenoxylate
w/ atropine = Lomotil |
Peripheral Mu Agonist
|
|
|
loperamide (Imodium)
|
Peripheral Mu Agonist
|
|
|
peragoric
|
Peripheral Mu Agonist
Antidiarrheal |
|
|
DTO (deodorized tincture of opium)
|
Peripheral Mu Agonist
|
|
|
naloxone (Narcon)
|
Mu Receptor Antagonist
|
|
|
naltrexone
|
Mu Receptor Antagonist
|
|
|
nalbuphine
|
Kappa agonist / Mu Antagonist
|
|
|
butorphanol
|
Kappa agonist / Mu Antagonist
|
|
|
pentazocine (Talwin)
|
Kappa agonist / Mu Antagonist
|
|
|
Talwin NX
(pentazocine + naloxone) |
Kappa agonist / Mu Antagonist
|
|
|
buprenorphine (subutex)
sublingual |
Mu Partial Agonist / Kappa antagonist
|
|
|
buprenorphine
w/ naloxone = (suboxone) |
Mu Partial Agonist / Kappa antagonist
|
|
|
Prialt (ziconotide)
|
Conotoxin
Block N-Type Calcium channels at dorsal horn- decreasing release of substance P and glutamate |
|
|
Conotoxin blocks ______ channels found on the dorsal horn decreasing:
|
N-type calcium channels
Decrease release of glutamate and substance P |
|
|
Benzodiazepines will ________ IPSPs
|
augment
|
|
|
Antiepileptics will _______ EPSPs
|
inhibit
|
|
|
GABAa and GABAc receptors are _______
|
ionotropic ligand gated
(influx Cl-) |
|
|
GABAb receptors are _______
|
metabotropic g-protein coupled
(K+ efflux) |
|
|
Glutamate receptors are_____
|
ionotropic ligand gated
(AMPA,NMDA) |
|
|
Therapeutic use of AMPA/NMDA receptor antagonists
|
Antiepileptics
|
|
|
α1 GABAa linked to
|
sedation / hypnosis
|
|
|
α2 / α3 GABAa linked to
|
anxiety
|
|
|
Benzodiazepines used for ________ because
|
both sedation and or anxiety
affinity for both α1 + α2 GABAa receptors |
|
|
Benzodiazepine - like drugs are only used for sedation because
|
They are more selective for α1 GABAa
|
|
|
BDZs have a safety advantage over barbituates because
|
they are positive allosteric modulators with no agonist effect like barbituates
|
|
|
Midazolam (Versed; IV,IM)
|
Short Acting Benzodiazepine
|
|
|
Triazolam (Halcion; oral)
|
Short Acting Benzodiazepine
|
|
|
Alprazolam (Xanax; oral)
|
Intermediate Acting Benzodiazepine
|
|
|
Estazolam (Prosom; oral)
|
Intermediate Acting Benzodiazepine
(Insomnia) |
|
|
Lorazepam (Ativan; oral, IV, IM)
|
Intermediate Acting Benzodiazepine
|
|
|
Oxazepam (Serax; oral)
|
Intermediate Acting Benzodiazepine
|
|
|
Temazepam (Restoril; oral)
|
Intermediate Acting Benzodiazepine
|
|
|
Chlordiazepoxide
(Librium; oral, IM, IV) |
Long Acting Benzodiazepine
|
|
|
Clonazepam (Klonopin; oral)
|
Long Acting Benzodiazepine
|
|
|
Clorazepate (Tranxene; oral)
|
Long Acting Benzodiazepine
|
|
|
Diazepam (Valium; oral,
IM, IV and PR (Diastat)) |
Long Acting Benzodiazepine
|
|
|
Flurazepam (Dalmane; oral)
|
Long Acting Benzodiazepine
|
|
|
Quazepam (Doral; oral)
|
Long Acting Benzodiazepine
(Insomnia) |
|
|
_______ acting benzodiazepines have active metabolites
|
Long
|
|
|
Non-CYP benzo substrates
(glucuronidation) |
Lorazepam
Oxazepam Temazepam |
|
|
Zaleplon (Sonata; oral)
|
Benzodiazepine related drug
|
|
|
Zolpidem (Ambien; oral)
|
Benzodiazepine related drug
|
|
|
Eszopiclone (Lunesta; oral)
|
Benzodiazepine related drug
|
|
|
Flumazenil (Romazicon) IV
|
Benzodiazepine antidote
(GABAa antagonist) |
|
|
AMPA receptor is:
|
Ligand Gated Sodium ion channel
|
|
|
Glutamate binds AMPA receptor causing _______ whereas Barbituates ________
|
Na+ influx
Block influx |
|
|
Thiopental (Pentothal; IV)
|
Ultra-short acting barbiturate
|
|
|
Methohexital (Brevital; IV)
|
Ultra-short acting barbiturate
|
|
|
Pentobrabital (Nembutal; IV, IM)
|
Ultra-short acting barbiturate
|
|
|
Amobarbital (Amytal; IV, IM)
|
Short Acting barbiturate
|
|
|
Butabrabital (Butisol;oral)
|
Short Acting barbiturate
|
|
|
Butalbital (Fioricet,
Fiorinal; oral) in combination with caffeine, acetaminophen or aspirin |
Short Acting barbiturate
|
|
|
Mephobarbital (Mebaral; oral)
|
Short Acting barbiturate
|
|
|
Secobarbital (Seconal; oral)
|
Short Acting barbiturate
|
|
|
Phenobarbital (Luminal; oral, IM, IV)
|
Long Acting barbiturate
(Anticonvulsant, Epilepsy, pre-op) |
|
|
Chronic use of barbiturates will upregulate ________ enzymes
|
CYP3A4
CYP3A5 CYP3A7 |
|
|
How to treat a barbiturate overdose
|
Alkalinizing urine with sodium bicarbonate + normal saline
|
|
|
Ramelteon (Rozerem)
|
Melatonin receptor agonist
|
|
|
Buspirone (Buspar)
|
Serotonin 5-HT1a Receptor Partial Agonist
Anxiolytic |
|
|
Dantrolene and BOTOX act ________ to relax muscles
|
Peripherally
|
|
|
Baclofen
|
GABAb Agonist
spasticity |
|
|
Tizanidine
|
alpha 2 agonist
muscle relaxant |
|
|
GABA at GABAb receptors MOA:
|
Inhibit Ca++ Entry presynapse
Stimulate K+ Efflux postsynapse |
|
|
Cyclobenzaprine (Flexeril)
|
Muscle Relaxant
5-HT2 Agonist + TCA = decrease alpha2 motor neuron stimulation |
|
|
Methocarbamol (Robaxin)
|
Muscle Relaxant
|
|
|
Carisopradol (Soma)
|
Muscle Relaxant
|
|
|
Orphenadrine (Norflex)
|
Muscle Relaxant
|
|
|
phenytoin (Dilantin) oral,IV
|
Na+ Channel Antagonist
antiepileptic |
|
|
fosphenytoin (Cerebyx) IV,IM
|
Na+ Channel Antagonist
antiepileptic prodrug |
|
|
carbamazepine (Tegretol)
|
Na+ Channel Antagonist
|
|
|
oxcarbazepine (Trileptal)
|
Na+ Channel Antagonist
|
|
|
lamotrigine (Lamictal)
|
Na+ Channel Antagonist
inhibits neuronal glutamate release |
|
|
_____ calcium channels in the thalamus are responsible for absence seizures
|
Transient Type
|
|
|
Ethosuximide (Zarontin)
|
T-type Ca channel antagonist
(Absence Seizures) |
|
|
Zonisamide (Zonegran)
|
T-type Ca channel antagonist
Na+ Channel Antagonist |
|
|
Gabapentin (Neurontin)
|
Reduces Ca influx mediated neurotransmitter release
Glu,NE,DA,substance P |
|
|
Pregabalin (Lyrica)
|
Reduces Ca influx mediated neurotransmitter release
Glu,NE,DA,substance P |
|
|
Tiagabine (Gabitril)
|
GAT-1 Inhibitor
Antiepileptic |
|
|
Vigabatrin (Sabril)
|
Irreversible GABA-T inhibitor
|
|
|
Valproic Acid (Divalproex (oral; Depakote), Valproic acid
(Oral; Depakene), Sodium Valproate (I.V.) |
Na+ Channel Antagonist
T-type Ca channel antagonist Enhancing GABA transmission via increase in GAD |
|
|
Levetiracetam (Keppra)
|
Inhibition of High-voltage gated Ca channels
Inhibition of excitatory neurotransmitter release Reversal of zinc-induced inhibition of GABAa receptor |
|
|
Topiramate
|
AMPA Receptor Antagonist
|
|
|
Felbamate (Felbatol)
|
NMDA Receptor Antagonist
|
|
|
Isoflurane
|
Inhalational Anesthetic
|
|
|
Enflurane
|
Inhalational Anesthetic
|
|
|
Desflurane
|
Inhalational Anesthetic
|
|
|
Sevoflurane
|
Inhalational Anesthetic
|
|
|
Halothane
|
Inhalational Anesthetic
|
|
|
Nitrous Oxide
|
Inhalational Anesthetic
(NMDA antagonist) |
|
|
Thiopental
|
Intravenous Anesthetic
|
|
|
Propofol
|
Intravenous Anesthetic
|
|
|
Etomidate
|
Intravenous Anesthetic
|
|
|
Ketamine
|
Intravenous Anesthetic
|
|
|
Thought to exert non-specific effect on plasma membrane of excitable neurons leading to stabilization of hyperpolarized state
|
Inhalation Anesthetics
|
|
|
Inhalational anesthetic % volume of inspired air at
which 50% of patients do not respond to a surgical stimulus |
Minimum alveolar concentration
|
|
|
Higher oil:gas partition =
_____ MAC = _______ potency |
lower MAC
Higher potency |
|
|
Blood : gas partitioning < 1 = _________ induction rate
|
fast
Agents with low solubility in blood quickly saturate the blood. The additional anesthetic molecules are then readily transferred to the brain |
|
|
Rare complication of inhalational general anesthetics, and
depolarizing neuromuscular blockers |
Malignant Hyperthermia
Increased release of calcium from sarcoplasmic reticulum |
|
|
True or False
intravenous anesthetics may lead to malignant hyperthermia |
False
|
|
|
Dantrolene
|
Direct Acting Muscle Relaxant
|
|
|
Dantrolene MOA
|
Inhibits release of Ca2+ release from sarcoplasmic reticulum by binding to ryanodine receptor
|
|
|
Propofol (Diprivan) MOA
|
Voltage gated Na+ channel antagonist
Targets GABAa receptors |
|
|
Fospropofol
|
Phosphate ester prodrug of propofol given as a solution to avoid emulsion allergy
|
|
|
Ketamine (Ketalar) MOA
|
NMDA noncompetitive antagonist
alpha1 + beta1 agonist Prevents reuptake of catecholamines |
|
|
Major AE of ketamine
|
Dissociative anesthesia
Delirium, hallucinations, unpleasant dreams |
|
|
Analgesic effect + trance-like cataleptic unconscious state
|
Dissociative anesthesia
|
|
|
Etomidate (Amidate) MOA
|
GABAa Agonist
Decreased cerebral flow ICP with minimal effect on CO HR and MAP |
|
|
AE associated with etomidate
|
Adrenal insufficiency inhibiting glucocorticoid and mineralcorticoid synthesis
|
|
|
Serotonin is derived from ________ via ________ hydroxylase
|
tryptophan
|
|
|
5-HT1b
|
Vessels - constriction
|
|
|
5-HT1d
|
Autoreceptor
|
|
|
5-HT2a
|
Platelets
|
|
|
5-HT2c
|
heart valves
|
|
|
5-HT3 + 5-HT4
|
GIT - increase motility
|
|
|
All serotonin receptor subtypes are G-protein coupled except
|
5-HT3 ligand gated
|
|
|
Stimulation of the trigeminal nerve releases ______ onto ____ cells leading to inflammation. ______ dilates cerebral vessels causing;
|
CGRP
mast cells CGRP pain associated with migraines |
|
|
Possible reason for the cause of an aura associated with migraines
|
Dilation of blood vessels in brain causing blood to pool in certain areas.
|
|
|
During a migraine ________ acts as a neurotransmitter in the transmission of pain impulses to the thalamus.
|
CGRP
|
|
|
sumatriptan (Imitrex)
|
5-HT1b + 5-HT1d Agonist
Abortive migraine therapy |
|
|
almotriptan (Axert)
|
5-HT1b + 5-HT1d Agonist
Abortive migraine therapy |
|
|
zolmitriptan (Zomig)
|
5-HT1b + 5-HT1d Agonist
Abortive migraine therapy |
|
|
naratriptan (Amerge)
|
5-HT1b + 5-HT1d Agonist
Abortive migraine therapy |
|
|
rizatriptan (Maxalt)
|
5-HT1b + 5-HT1d Agonist
Abortive migraine therapy |
|
|
frovatriptan (Frova)
|
5-HT1b + 5-HT1d Agonist
Abortive migraine therapy |
|
|
eletriptan (Relpax)
|
5-HT1b + 5-HT1d Agonist
Abortive migraine therapy |
|
|
ergotamine
|
Ergot abortive migraine therapy
|
|
|
dihydroergotamine
|
Ergot abortive migraine therapy
|
|
|
Methergine (methylergonovine)
|
Ergot abortive migraine therapy
|
|
|
bromocriptine
|
Ergot abortive migraine therapy
Parkinson's - not usually Hyperprolactemia |
|
|
Preventative options for migraines:
|
Propranolol
Verapamil Divalproex, topiramate ACE inhibitors, ARBs BOTOX |
|
|
Ergotism =
Treatment = |
Severe vasoconstriction with possible gangrene when untreated
Nitroprusside |
|
|
Due to their non-selectivity ________ stimulate the chemotrigger zone when treating migraines.
|
Ergots
nausea vomiting |
|
|
NSAIDs, aspirin, acetaminophen
- Treximet = sumatriptan + naproxen |
Abortive migraine therapy
|
|
|
Fiorinal or Fioricet
- Aspirin or acetaminophen, plus butalbital plus caffeine |
Abortive migraine therapy
|
|
|
True or False
NE neurons and Serotonergic neurons both contain vmat |
True
|
|
|
Adderall
|
Amphetamine
Indirect-acting sympathomimetic |
|
|
Dexedrine (dextroamphetamine) (d-isomer)
|
Amphetamine
Indirect-acting sympathomimetic |
|
|
Desoxyn (methamphetamine)
|
Amphetamine
Indirect-acting sympathomimetic |
|
|
Vyvanse (lisdexamfetamine)
|
Amphetamine
Indirect-acting sympathomimetic |
|
|
Ritalin
|
Methylphenidate
Indirect-acting sympathomimetic |
|
|
Concerta
|
Methylphenidate
Indirect-acting sympathomimetic |
|
|
Focalin (dexmethylphenidate)
|
Methylphenidate
Indirect-acting sympathomimetic |
|
|
ADD/ ADHD
_______ displace monoamines from vesicles by physically entering them |
Amphetamines
|
|
|
ADD / ADHD
________ block NET preventing reuptake of NE, building a concentration at the synapse |
Methylphenidates
|
|
|
benzphetamine (Didrex)
|
Indirect Sympathomimetic
|
|
|
diethylpropion
|
Indirect Sympathomimetic
|
|
|
phendimetrazine
|
Indirect Sympathomimetic
|
|
|
Provigil (modafinil)
|
Indirect Sympathomimetic
|
|
|
Nuvigil (armodafinil)
|
Indirect Sympathomimetic
|
|
|
ephedrine
|
Indirect Sympathomimetic
|
|
|
Strattera (atomoxetine)
|
Indirect Sympathomimetic
NARI (2D6 deficiency must decrease dose) |
|
|
imipramine
|
Tricyclic Antidepressant
|
|
|
desipramine
|
Tricyclic Antidepressant
|
|
|
clomipramine (Anafranil)
|
Tricyclic Antidepressant
|
|
|
amitriptyline
|
Tricyclic Antidepressant
|
|
|
fluvoxamine
|
SSRI
|
|
|
Paroxetine (Paxil)
|
SSRI
|
|
|
Fluoxetine (Prozac)
|
SSRI
|
|
|
venlafaxine (Effexor)
|
SNRI
|
|
|
desvenlafaxine (Pristiq)
|
SNRI
|
|
|
duloxetine (cymbalta)
|
SNRI
|
|
|
milnacipran (Savella)
|
SNRI
|
|
|
phenelzine (Nardil)
|
MAOI
|
|
|
tranylcypromine (Parnate)
|
MAOI
|
|
|
selegiline (Anipryl)
|
MAO-b inhibitor
|
|
|
bupropion (Wellbutrin)
|
Atypical antidepressant
|
|
|
mirtazapine (Remeron)
|
Atypical antidepressant
|
|
|
nefazadone
|
Atypical antidepressant
|
|
|
trazadone
|
Atypical antidepressant
|
|
|
chlorpromazine (Thorazine)
|
Typical Antipsychotic
|
|
|
thioridazine (Mellaril)
|
Typical Antipsychotic
(QTC prolongation) |
|
|
fluphenazine (Prolixin)
|
Typtical Antipsychotic
|
|
|
perphenazine (Trilafon)
|
Typtical Antipsychotic
|
|
|
trifluoperazine
|
Typtical Antipsychotic
|
|
|
thiothixene (Navane)
|
Typtical Antipsychotic
|
|
|
haloperidol (Haldol)
|
Typtical Antipsychotic
|
|
|
molindone
|
Typtical Antipsychotic
|
|
|
loxapine
|
Typtical Antipsychotic
|
|
|
pimozide (orap)
|
Typical Antipsychotic
Tourettes syndrome |
|
|
aripiprazole (Abilify)
|
Atypical Antipsychotic
|
|
|
clozapine (Clozaril)
|
Atypical Antipsychotic
|
|
|
clanzapine (Zyprexa)
|
Atypical Antipsychotic
|
|
|
quetiapine (Seroquel)
|
Atypical Antipsychotic
|
|
|
resperidone (Risperdal)
|
Atypical Antipsychotic
|
|
|
ziprasidone (Geodon)
|
Atypical Antipsychotic
|
|
|
paliperidone (Invega)
|
Atypical Antipsychotic
|
|
|
lurasidone (Latuda)
|
Atypical Antipsychotic
|
|
|
olanzapine + fluoxetine (Symbyax)
|
Atypical Antipsychotic
|
|
|
Levodopa
|
Dopamine Agonist
|
|
|
Carbidopa
|
DOPA decarboxylase inhibitor
|
|
|
Sinemet
|
levodopa + carbidopa
|
|
|
tolcapone (tasmar)
|
COMT inhibitor
|
|
|
entacapone (comtan)
|
COMT inhibitor
|
|
|
stalevo
|
levodopa + carbidopa + entacapone
|
|
|
Besides migraines: bromocriptine and carbergoline are used for
|
Dopamine Receptor Agonist
Hyperprolactinemia |
|
|
ropinerole (requip)
|
Dopamine Receptor Agonist
|
|
|
pramipexole (mirapex)
|
Dopamine Receptor Agonist
|
|
|
apomorphine
|
Dopamine Receptor Agonist
subcutaneous emergency use w/ antiemetics |
|
|
selegiline (eldepryl)
|
MAO-B inhibitor
|
|
|
rasagiline (azilect)
|
MAO-B inhibitor
|
|
|
ensam
|
selegiline patch
depression |
|
|
amantadine
|
Dopamine Releasing Agent
NMDA antagonist |
|
|
tacrine (cognex)
|
Central Cholinesterase Inhibitor
very toxic - not used |
|
|
donepizil (Aricept)
|
Central Cholinesterase Inhibitor
Alzheimer's |
|
|
rivastigmine (exelon)
|
Central Cholinesterase Inhibitor
Alzheimer's |
|
|
galantamine (razadyne)
|
Central Cholinesterase Inhibitor
Alzheimer's |
|
|
namenda (memantine)
|
Glutamate NMDA Antagonist
Alzheimer's |
|
|
riluzole (rilutek)
|
Glutamate NMDA Antagonist
ALS |
|
|
Ceftriaxone
|
Third Gen Cephalosporin
Increases glutamate reuptake transporters on astrocytes ALS |
|
|
11-B-hydroxysteroid dehydrogenase
|
converts cortisol to cortisone decreasing aldosterone-like effects on kidney
|
|
|
fludrocortisone (florinef)
|
Mineralocorticoid Agonist
Na retention, water retention |
|
|
cortisol
|
Glucocorticoid Receptor Agonist
GR > MR |
|
|
prednisone
|
Glucocorticoid Receptor Agonist
GR > MR |
|
|
prednisilone
|
Glucocorticoid Receptor Agonist
GR > MR |
|
|
cortisone
|
Glucocorticoid Receptor Agonist
GR > MR |
|
|
methylprednisolone
|
Glucocorticoid Receptor Agonist
GR > MR |
|
|
triamcinolone
|
Glucocorticoid Receptor Agonist
GR > > > MR |
|
|
betamethasone
|
Glucocorticoid Receptor Agonist
GR > > > MR |
|
|
dexamethasone
|
Glucocorticoid Receptor Agonist
GR > > > MR |
|
|
CRF (achthrel)
|
Glucocorticoid Receptor Agonist
|
|
|
ACTH (cosyntropin)
|
Corticosteroid Agonist
|
|
|
trilostane
|
Cortisol Synthesis Inhibitor
Cushings Syndrome |
|
|
aminoglutethimide
|
Cortisol Synthesis Inhibitor
(Cushings Syndrome) Aromatase Inhibitor (Breast Cancer) |
|
|
metyrapone
|
Cortisol Synthesis Inhibitor
Cushings Syndrome |
|
|
ketoconazole
|
Cortisol Synthesis Inhibitor
Cushings Syndrome |
|
|
Interferon-beta (Avonex, Rebif, Betaseron)
|
Disease Modifying Immunosuppressant
Multiple Sclerosis |
|
|
glatiramer acetate (Copaxone)
|
Disease Modifying Immunosuppressant
Multiple Sclerosis |
|
|
natalizumab (Tysabri)
|
Disease Modifying Immunosuppressant
Multiple Sclerosis |
|
|
dalfampridine (Ampyra)
|
Blocks K+ efflux from demyelinated segments to improve conduction
Multiple Sclerosis |
|
|
fingolimod (Gilenya)
|
Disease Modifying Immunosuppressant
Multiple Sclerosis |
|
|
mitoxantrone (novantrone)
|
Antineoplastic Agent
Secondary Progressive MS |
|
|
cyclosporine (sandimmune, restasis)
|
Immunosuppressant
|
|
|
tacrolimus (Prograf, Protopic)
|
Immunosuppressant
|
|
|
pimecrolimus (Elidel)
|
Immunosuppressant
|
|
|
sirolimus (Rapamune)
|
Immunosuppressant
|
|
|
azothioprine (Imuran)
|
Immunosuppressant
|
|
|
mycophenolate mofetil (Cellcept, Myfortic)
|
Immunosuppressant
Purine Synthesis Inhibitor |
|
|
daclizumab
|
Immunosuppressant
MAB against IL-2 |
|
|
basiliximab
|
Immunosuppressant
MAB against IL-2 - block cell cycle |
|
|
muromonab-CD3
|
Immunosuppressant
Acute organ transplant |
|
|
methotrexate
|
Traditional DMARD
purine synthesis inhibitor |
|
|
leflunomide (Arava)
|
Traditional DMARD
pyrimidine synthesis inhibition |
|
|
sulfasalazine
|
Traditional DMARD
+IBD |
|
|
hydroxyqloroquine (Plaquenil)
|
Traditional DMARD
|
|
|
gold (auranofin, solganol)
|
Traditional DMARD
|
|
|
penicillamine
|
Traditional DMARD
Used to chelate copper in Wilsons Disease |
|
|
azothioprine (Imuran)
|
Immunosuppressant, Traditional DMARD
(prodrug of 6-MP) |
|
|
cyclosporine
|
Immunosuppressant, Traditional DMARD
|
|
|
enbrel (etanercept)
|
TNFα Antagonist
Biological DMARD |
|
|
remicade (infliximab)
|
TNFα Antagonist
Biological DMARD |
|
|
Humira (adalmumab)
|
TNFα Antagonist
Biological DMARD |
|
|
cimzia (certolizumab)
|
TNFα Antagonist
Biological DMARD |
|
|
simponi (golimumab)
|
TNFα Antagonist
Biological DMARD |
|
|
kineret
|
IL-1 Receptor Antagonist
|
|
|
actemra
|
Biological DMARD
IL-6 Receptor Antagonist |
|
|
orencia
|
Biological DMARD :Fusion Protein
Binds CD80 + CD86 on B-Cell (Block antigen presenting) |
|
|
clomiphene (clomid)
|
SERM
Infertility |
|
|
menotropins
|
Exogenous Gonadotropins
(FSH + LH) Infertility |
|
|
gonadorelin
|
Synthetic GnRH
Infertility |
|
|
ganirelix
|
GnRH Antagonist
Given with exogenous FSH to ensure maturation of follicles before premature LH surge Infertility, cancer |
|
|
cetrorelix
|
GnRH Antagonist
Given with exogenous FSH to ensure maturation of follicles before premature LH surge Infertility, cancer |
|
|
How can estrogen be used to treat acne?
|
Acne is an androgenic effect. Estrogen will activate testosterone binding protein nuclear hormone receptor, reducing the amount of active androgen.
|
|
|
For contraception, estrogens work through _________ while progestins work by _________
|
Negative feedback inhibition of gonadotropins.
Thick mucus secretion on endometrium to inhibit fertilization and prevent implantation. |
|
|
Monophasic combination OCs have fixed amounts of estrogens and progestins, while biphasic and triphasic OCs have fixed amounts of ________ but start off low with ________.
|
Estrogen
Progestin |
|
|
Minipill
|
Progestin only
|
|
|
ethinyl estradiol
|
estrogen
|
|
|
mestranol
|
estrogen
|
|
|
norgestimate
|
progestin
|
|
|
medroxyprogesterone
|
progestin
|
|
|
norgestrel
|
progestin
|
|
|
levonorgestrel
– Plan B |
progestin
|
|
|
norethindrone
|
progestin
|
|
|
ethynodiol
|
progestin
|
|
|
desogestrel
|
progestin
|
|
|
drosperinone
|
progestin
|
|
|
mifepristone (RU-486)
|
Progesterone receptor antagonist
|
|
|
______ and ______ are the most androgenic progestins
|
norgestrel + levonorgestrel
|
|
|
testosterone (depo-testosterone, androderm, androgel)
|
androgen
hypogonadism, post menopause, male senescence |
|
|
methyltestosterone
|
androgen
hypogonadism, post menopause, male senescence |
|
|
danocrine (Danazol)
|
androgen
endometriosis |
|
|
fluoxymestrone (Halotestin)
|
Anabolic steroid
|
|
|
oxandrolone
|
Anabolic steroid
|
|
|
oxymetholone
|
Anabolic steroid
|
|
|
stanozolol (Winstrol)
|
Anabolic steroid
|
|
|
nandrolone (Deca Durabolin)
|
Anabolic steroid
|
|
|
Abarelix
|
GnRH receptor antagonist
prostate cancer |
|
|
Why do GnRH antagonists and agonists have the same effect?
|
GnRH is released in a pulsating manner, agonists will activate GnRH at first but downregulate receptor over time.
|
|
|
leuprolide (Lupron)
|
GnRH Receptor Agonist
prostate / breast cancer endometriosis precocious puberty |
|
|
nafarelin
|
GnRH Receptor Agonist
prostate / breast cancer endometriosis precocious puberty |
|
|
goserelin
|
GnRH Receptor Agonist
prostate / breast cancer endometriosis precocious puberty |
|
|
buserelin
|
GnRH Receptor Agonist
prostate / breast cancer endometriosis precocious puberty |
|
|
histrelin
|
GnRH Receptor Agonist
prostate / breast cancer endometriosis precocious puberty |
|
|
triptorelin
|
GnRH Receptor Agonist
prostate / breast cancer endometriosis precocious puberty |
|
|
finasteride (Propecia)
|
5-alpha reductase inhibitor
II > I anti-baldness |
|
|
finasteride (Proscar)
|
5-alpha reductase inhibitor
II > I BPH |
|
|
duasteride
|
5-alpha reductase inhibitor
nonselective anti-baldness, BPH |
|
|
Why can't androgen receptor antagonists be used in later stages of prostate cancer?
|
Cancer growth is no longer dependent on androgen.
|
|
|
flutamide (Eulexin)
|
Androgen Receptor Antagonist
prostate cancer |
|
|
bicalutamide (Lasodex)
|
Androgen Receptor Antagonist
prostate cancer |
|
|
nilutamide (Nilandron)
|
Androgen Receptor Antagonist
prostate cancer |
|
|
Why may androgen receptor antagonists be more efficacious for prostate cancer when compared to GnRH receptor antagonists / agonists
|
The adrenal gland can still produce testosterone so blocking at the androgen receptors allows for more complete blockade.
|
|
|
somatropin
|
Recombinant GH
|
|
|
somatrem
|
Recombinant GH
|
|
|
sermorelin
|
Synthetic GHRH
|
|
|
Recombinant IGF-1 effects:
|
lipolysis, increase size, increase bone length / density, decrease glucose
|
|
|
octreotide (Sandostatin)
|
Recombinant GH Antagonist
Somatostatin-5 Agonist (SST-5 Agonist) acromegaly, GI bleeds (constriction) |
|
|
pegvisomant (Somavert)
|
Recombinant GH Antagonist
SST-5 Agonist Acromegaly |
|
|
Sermorelin is more effective for this indication rather than GH deficiency
|
To test for pituitary dysfunction
|
|
|
Before surgery is an option, ________ or ________ can be used to treat acromegaly
|
octreotide (Sandostatin)
pegvisomant (Somavert) GH inhibitors |
|
|
raloxifene
|
SERM / Anti-resorptive Drug
osteoporosis |
|
|
estrogens can be used to ________ osteoclast activity
|
decrease
|
|
|
Alendronate (Fosamax)
|
Bisphosphonate
osteoporosis |
|
|
Risedronate (Actonel)
|
Bisphosphonate
osteoporosis |
|
|
Ibandronate (Boniva)
|
Bisphosphonate
osteoporosis |
|
|
Calitonin is release from the ________ when calcium levels are too _____
|
thyroid
high |
|
|
miacalcitonin
|
Salmon Calcitonin
osteoporosis |
|
|
________ is released when calcium levels are too low
|
parathyroid hormone
|
|
|
Teriparatide (Forteo)
|
Recombinant fragment of parathyroid hormone
Paradoxical effect: Increase osteoblast activity 2 year use only - cancer risk |
|
|
lispro (Humalog)
|
Rapid Acting Insulin
|
|
|
aspart (Novolog)
|
Rapid Acting Insulin
|
|
|
glulisine (Apidra)
|
Rapid Acting Insulin
|
|
|
Humulin R, Novolin R
|
Short Acting Regular Insulin
|
|
|
Humulin N, Novolin N
|
Protamine complexed intermediate acting insulin
|
|
|
glargine (Lantus)
|
Long Acting Insulin
|
|
|
detemir (Levemir)
|
Long Acting Insulin
|
|
|
pramlintide (Symlin)
|
Synthetic Amylin
Slows gastric emptying rate and absorption of glucose Decreases release of glucagon from pancreas |
|
|
Metformin therapeutic effects:
|
Activates AMP Kinase working to reduce gluconeogenesis in liver
Increase fatty acid oxidation to increase sensitivity to insulin in body Reduces appetite |
|
|
pioglitazone (Actos)
|
Thiazolidinedione
PPAR Agonist Increase insulin sensitivity |
|
|
rosiglitazone (Avandia)
|
Thiazolidinedione
PPAR Agonist Increase insulin sensitivity |
|
|
acarbose (Precose)
|
α Glucosidase Inhibitor
Slows breakdown of starches to glucose in intestine to balance absorption |
|
|
miglitol (Glyset)
|
α Glucosidase Inhibitor
Slows breakdown of starches to glucose in intestine to balance absorption |
|
|
chlorpropamide
|
Secretagogue: Sulfonylurea
Block K+ channel mimicking ATP in beta cell to increase insulin secretion May block glucagon + glucose release from liver |
|
|
glyburide (Micronase)
|
Secretagogue: Sulfonylurea
Block K+ channel mimicking ATP in beta cell to increase insulin secretion May block glucagon + glucose release from liver |
|
|
glipizide (Glucotrol)
|
Secretagogue: Sulfonylurea
Block K+ channel mimicking ATP in beta cell to increase insulin secretion May block glucagon + glucose release from liver |
|
|
glimepiride (Amaryl)
|
Secretagogue: Sulfonylurea
Block K+ channel mimicking ATP in beta cell to increase insulin secretion May block glucagon + glucose release from liver |
|
|
repaglinide (Prandin)
|
Secretagogue: Meglitinide
Block K+ channel mimicking ATP in beta cell to increase insulin secretion May block glucagon + glucose release from liver |
|
|
natelinide (Starlix)
|
Secretagogue: Meglitinide
Block K+ channel mimicking ATP in beta cell to increase insulin secretion May block glucagon + glucose release from liver |
|
|
exenatide (Byetta)
|
GLP-1 Agonist
type 2 DM |
|
|
liraglutide (Victoza)
|
GLP-1 Agonist
type 2 DM |
|
|
sitagliptin (Januvia)
|
DPP-IV Inhibitor
prevents GLP-1 breakdown |
|
|
saxagliptin (Onglyza)
|
DPP-IV Inhibitor
prevents GLP-1 breakdown |
|
|
raloxifene (Evista)
|
SERM
osteoporosis |
|
|
tamoxifen (Nolvadex)
|
SERM
breast cancer |
|
|
toremifene (Fareston)
|
SERM
breast cancer |
|
|
Fulvestrant (Faslodex)
|
SERD
breast cancer |
|
|
estradiol
– Estrace – Climara, Vivelle |
Estrogen agonist HRT
post menopause |
|
|
estrogens conjugated (premarin)
|
Estrogen agonist HRT
post menopause |
|
|
Prempro
|
Combination estrogen / progestin HRT
post menopause |
|
|
progesterone (Prometrium)
|
Progesterone HRT
prevent endometrial hyperplasia |
|
|
Femhrt
|
Combination estrogen / progestin HRT
post menopause |
|
|
Medroxyprogesterone Acetate (Provera)
|
Progestin HRT
prevent endometrial hyperplasia |
|
|
Climara Pro
|
Combination estrogen / progestin HRT
menopause |
|
|
Combipatch
|
Combination estrogen / progestin HRT
menopause |
|
|
Norethindrone (Aygestin)
|
Progestin Agonist HRT / contraceptive
|
|
|
estrone or estropiprate (Ogen)
|
Estrogen Agonist HRT
postmenopause |
|
|
esterified estrogens (Menest)
|
Estrogen Agonist HRT
postmenopause |
|
|
synthetic conjugated estrogens (Cenestin, Enjuvia)
|
Estrogen Agonist HRT
postmenopause |
|
|
estrogen
– Vagifem – Estring, Femrin |
Estrogen Agonist HRT
postmenopause |
|
|
Levothyroxine (Synthroid)
|
Tetraiodothyronine (T4)
Hypothyroidism / Myxedema |
|
|
Liothyronine (Cytomel)
|
Triiodothyronine (T3)
Hypothyroidism / Myxedema |
|
|
Liotrix (Thyrolar)
|
T4 + T3 mix
Hypothyroidism / Myxedema |
|
|
propylthiouracil (PTU)
|
Thioperoxidase Inhibitor
Hyperthyroidism |
|
|
methimazole
|
Thioperoxidase Inhibitor
Hyperthyroidism |
|
|
Thiocyanate
|
Iodide Pump Inhibitor
Hyperthyroidism |
|
|
Perchlorate
|
Iodide Pump Inhibitor
Hyperthyroidism |
|
|
High dose iodide will ________ thyroid activity
|
decrease!
|
|
|
Lugols Solution
|
Iodide
Hyperthyroidism |
|
|
SSKI
|
Iodide
Hyperthyroidism |
|
|
131 I
|
Radioactive iodide
Destroys cells in thyroid |
|
|
Instead of psychosis, short term use of these D2 antagonists are indicated as anti-emetics
|
prochlorperazine (Compazine)
trimethobenzamide (Tigan) promethazine (Phenergan) |
|
|
ondansetron (Zofran)
|
5-HT3 Antagonist
Anti-emetic |
|
|
granisetron (Kytril)
|
5-HT3 Antagonist
Anti-emetic |
|
|
dolansetron (Anzemet)
|
5-HT3 Antagonist
Anti-emetic |
|
|
polonosetron (Aloxi)
|
5-HT3 Antagonist
Anti-emetic |
|
|
aprepitant / fosprepitant (Emend)
|
NK1 Receptor Antagonist
Anti-emetic |
|
|
True or False
Emend is a good option to help stop someone from vomiting |
False - only work pre-vomit
|
|
|
dronabinol (Marinol)
|
CB1 Agonist
Anti-emetic |
|
|
nabilone (Cesamet)
|
CB1 Agonist
Anti-emetic |
|
|
alosetron (Lotronex)
|
5-HT3 Antagonist
works in colon to prevent diarrhea IBS in women |
|
|
lubiprostone (Amitiza)
|
Opens Cl- ions in GIT aiding in motility for constipation IBS
|
|
|
Because H.Pylori can be the cause of gastric ulcers, common drugs include
|
Amoxicillin
Azithromycin Metronidazole |
|
|
misoprostol (Cytotec)
|
PGE1 Receptor Agonist
Anti-ulcer |
|
|
sucralfate
|
Sucrose w/ sulfate + charge attracts and coats - charged ulceration for protection
|
|
|
cimetidine (Tagamet)
|
H2 Receptor Antagonist
|
|
|
alosetron (Lotronex)
|
5-HT3 Antagonist
works in colon to prevent diarrhea IBS in women |
|
|
ranitidine (Zantac)
|
H2 Receptor Antagonist
|
|
|
lubiprostone (Amitiza)
|
Opens Cl- ions in GIT aiding in motility for constipation IBS
|
|
|
nizatidine (Axid)
|
H2 Receptor Antagonist
|
|
|
Because H.Pylori can be the cause of gastric ulcers, common drugs include
|
Amoxicillin
Azithromycin Metronidazole |
|
|
famotidine (Pepcid)
|
H2 Receptor Antagonist
|
|
|
misoprostol (Cytotec)
|
PGE1 Receptor Agonist
Anti-ulcer |
|
|
omeprazole (Prilosec)
|
Proton pump inhibitor
|
|
|
sucralfate
|
Sucrose w/ sulfate + charge attracts and coats - charged ulceration for protection
|
|
|
cimetidine (Tagamet)
|
H2 Receptor Antagonist
|
|
|
ranitidine (Zantac)
|
H2 Receptor Antagonist
|
|
|
nizatidine (Axid)
|
H2 Receptor Antagonist
|
|
|
famotidine (Pepcid)
|
H2 Receptor Antagonist
|
|
|
omeprazole (Prilosec)
|
Proton pump inhibitor
|
|
|
esomeprazole (Nexium)
|
Proton pump inhibitor
|
|
|
lansoprazole (Prevacid)
|
Proton pump inhibitor
|
|
|
dexlansoprazole (Kapidex)
|
Proton pump inhibitor
|
|
|
rabeprazole (Aciphex)
|
Proton pump inhibitor
|
|
|
pantoprazole (Protonix)
|
Proton pump inhibitor
|
|
|
True or False
PPI's are pro-drugs |
True
|
|
|
xolair (omalizumab)
|
Anti-IgE
prevents degranulation of mast cells - decrease histamine |
|
|
cromolyn
|
Mast cell stabilizer
|
|
|
nedocromyl
|
Mast cell stabilizer
|
|
|
diphenhydramine (Benadryl)
|
1st Gen H1 Antagonist
|
|
|
clemastine (Tavist)
|
1st Gen H1 Antagonist
|
|
|
dimenhydrinate (Dramamine)
|
1st Gen H1 Antagonist
M1 antagonist - motion sickness |
|
|
chlorpheniramine (ChlorTrimeton)
|
1st Gen H1 Antagonist
|
|
|
brompheniramine
|
1st Gen H1 Antagonist
|
|
|
hydroxyzine (Atarax/Vistaril)
|
1st Gen H1 Antagonist
|
|
|
cyclizine
|
1st Gen H1 Antagonist
|
|
|
meclizine (Antivert)
|
1st Gen H1 Antagonist
|
|
|
promethazine (Phenergan)
|
1st Gen H1 Antagonist
D2 Antagonist |
|
|
cyproheptadine (Periactin)
|
1st Gen H1 Antagonist
(also blocks 5-HT2a to treat serotonin syndrome) |
|
|
Doxepin
|
1st Gen H1 Antagonist
|
|
|
loratidine (Claritin)
|
2nd Gen H1 Antagonist
|
|
|
desloratidine (Clarinex)
|
2nd Gen H1 Antagonist
|
|
|
cetirizine (Zyrtec)
|
2nd Gen H1 Antagonist
|
|
|
azelastine (Astelin)
|
2nd Gen H1 Antagonist
|
|
|
fexofenadine (Allegra)
|
2nd Gen H1 Antagonist
|
|
|
Procaine
|
Short Acting Local Anesthetic
|
|
|
Cocaine
|
Medium Acting Local Anesthetic
|
|
|
Prilocaine
|
Medium Acting Local Anesthetic
|
|
|
Mepivacaine
|
Medium Acting Local Anesthetic
|
|
|
Lidocaine
|
Medium Acting Local Anesthetic
|
|
|
Tetracaine
|
Long Acting Local Anesthetic
|
|
|
Bupivacaine
|
Long Acting Local Anesthetic
|
|
|
Ropivacaine
|
Long Acting Local Anesthetic
|
