Phamacology 2
Terms
undefined, object
copy deck
- Sumatriptan
-
U: Migraines
M: Agonists of 5-HT1D & 1B receptors
SE: Vasoconstiction of carotid and cranial
circulation
v cAMP & adenyl cyclase - Erogotamine
-
C: Ergot Amines
U: migraines
M: agonist & p. agonist of 5HT1D & 1A receptors
SE: vasoconstriction of carotid & cranial circulation
Decrease cAMP & adenyl cyclase - Alosetron
-
C:
U: Treat IBS
M: 5-HT3 antagonist
SE: diarrhea - Tegaserod
-
C:
U: IBS w/ Diarrhea
M: partial 5-HT4 agonist
-only for women - Odansteron
-
C:
U: Treat Nasea & Vomitting
M: 5-HT3 agonist - Strychnin
-
C: Toxin
U: Anxiolytic/Sedative/Hypnotic
M:comp anatagonist of glycine
SE: - Tetanus toxin
-
C: Toxin
U:
M: inhibits release of glycine - leads to excitation (full contraction of all voluntary muscles)
SE: - Thiopental
-
C:Barbituate
U:Sedative/Hypnotic
-GEN SEIZURES
-Esp for ANESTHESIA = *C-SECTIONS
-v O2 REQUIREMENT OF BRAIN
M:potentiates GABA; up duration of Cl- channel
SE: dependence, drowsiness, impaired congnition, confusion, depressed motor skills
v SNS, no chance in vasc r, resp depression, broncho/larygospasm, v mucociliary clearance
INDUCTION OF CYP450
SOME HISTAMINE RELEASE = hypotention
CONTRA:
pericardial tamponade
hypovolemia
CHF
Ischemic heart dz - Phenobarbital
-
C:Barbituate
U:Sedative/Hypnotic/
-General seizures
-Esp for EtOH dependence
M:potentiates GABA; up duration of Cl- channel
SE:dependence, drowsiness, impaired congnition, confusion, depressed motor skills
v SNS, no chance in vasc r, resp depression, broncho/larygospasm, v mucociliary clearance
INDUCTION OF CYP450 - Disulfiram
-
C:
U:treat alcohol abuse
M:block ADH
CONTRA: pregnancy, liver dz - Contra for all barbituates
-
-porphyria
-upper airway obstruction - Etomidate
-
C: Barbituate
U: esp used for pain & anticonvulsant
Special appeal = heart stability
SE: v cortisol syn
clonus on onset(major twiches)
v activity of A & B hydroxylases - Chlordiazepoxide
-
C:Benzodiazepine
U:Sedative/Hypnotic
LONG DURATION
M:potentiates GABA; up duration of Cl- channel
SE:dependence, drowsiness, impaired congnition, confusion, depressed motor skills - Diazepam
-
C: Benzodiazepine
U:Sedative/Hypnotic
ANTI-SPASM
STATUS EPILIPTICUS
M:potentiates GABA; up duration of Cl- channel
SE:dependence, drowsiness, impaired congnition, confusion, depressed motor skills
INSOLUBLE: SUPPLIED IN EMULSION - Lorazepam
-
C: Benzodiazepine
U:Sedative/Hypnotic
SHORT DURATION
STATUS EPILIPTICUS (1st line)
M:potentiates GABA; up duration of Cl- channel
SE:dependence, drowsiness, impaired congnition, confusion, depressed motor skills - Midazolam
-
C:Benzodiazepine
U:Sedative/Hypnotic
ANESTHESIA
PREFERRED IN OR b/c METABOLITE HAS NO EFFECTS
M:potentiates GABA; up duration of Cl- channel
SE:dependence, drowsiness, impaired congnition, confusion, depressed motor skills - Oxazepam
-
C: Benzodiazepine
U:Sedative/Hypnotic
VERY SHORT DURATION (faster than lorazapam)
STATUS EPILIPTICUS (1st line)
M:potentiates GABA; up duration of Cl- channel
SE:dependence, drowsiness, impaired congnition, confusion, depressed motor skills
VERY ACTIVE METABOLITE - For patients with liver injury, benzos or barbituates?
- Benzos, b/c barbituates induce CYP450 system
- Erogonovine, Methylergonovine
-
C: Ergot Alkyloids
U: poweful smooth muscle contractor
Treat Post-partum hemorrhage when oxytocin not effective
M:agonist of A-adrenergic receptors & 5-HT2 receptors
SE: - Methysergide
-
C: Ergot Alkyloids
U: poweful smooth muscle contractor
PROPHYLAXIS of MIGRAINE
M:Antagonist of 5-HT2A & 2C
SE: - Ketamine
-
C:
U:PRE-EMPTIVE ANALGESIA = minimizes need for post-op analgesia
v "wind up" effect (bruise doesnt hurt hours later)
M:
SE: excitement, hallucinations, flashbacks - Baclofen
-
C:
U:Anti-spasm (CNS)
M:acts as GABA agonist on afferent part of reflex arc
v release of excitatory NT
SE: - Flumazenil
-
C:Anxiogenic
U: Treat benzo OD
M: Benzo receptor antagonist (Cl- channel)
SE: Anxiety
-physostigmine (cholinesterase inhibitor) usually used before - Codeine
-
C: Opiod
U: Analgesic
M: MU, KAPPA, DELTA receptor agonist to block nociception
SE:dependence, constipation, nausea, vomiting, cough suppression, sedation, reduced urinary flow (and UTI)
OD: respiratory depression, coma, MIOSIS - Fentanyl
-
C: Opiod
U: Analgesic
PATCH - SLOW ONSET, LONG DURATION
M: MU, KAPPA, DELTA receptor agonist to block nociception
SE:dependence, constipation, nausea, vomiting, cough suppression, sedation, reduced urinary flow (and UTI)
OD: respiratory depression, coma, MIOSIS - Heroin
-
C: Opiod
U: Analgesic
M: MU, KAPPA, DELTA receptor agonist to block nociception
SE:dependence, constipation, nausea, vomiting, cough suppression, sedation, reduced urinary flow (and UTI)
OD: respiratory depression, coma, MIOSIS - Hydrocodone
-
C: Opiod
U: Analgesic
HIGHLY ABUSED
M: MU, KAPPA, DELTA receptor agonist to block nociception
SE:dependence, constipation, nausea, vomiting, cough suppression, sedation, reduced urinary flow (and UTI)
OD: respiratory depression, coma, MIOSIS - Hydromorphone
-
C: Opiod
U: Analgesic
M: MU, KAPPA, DELTA receptor agonist to block nociception
SE:dependence, constipation, nausea, vomiting, cough suppression, sedation, reduced urinary flow (and UTI)
OD: respiratory depression, coma, MIOSIS - Morphine
-
C: Opiod
U: Analgesic
M: MU, KAPPA, DELTA receptor agonist to block nociception
SE:dependence, constipation, nausea, vomiting, cough suppression, sedation, reduced urinary flow (and UTI)
OD: respiratory depression, coma, MIOSIS - Methadone
-
C: Opiod
U: Analgesic
USED TO TREAT OPIATE WITHDRAWALS
OFTEN ABUSED, PALLIATIVE
M: MU, KAPPA, DELTA receptor agonist to block nociception
SE:dependence, constipation, nausea, vomiting, cough suppression, sedation, reduced urinary flow (and UTI)
OD: respiratory depression, coma, MIOSIS - Oxycontin
-
C: Opiod
U: Analgesic
LONG DURATION
M: MU, KAPPA, DELTA receptor agonist to block nociception
SE:dependence, constipation, nausea, vomiting, cough suppression, sedation, reduced urinary flow (and UTI)
OD: respiratory depression, coma, MIOSIS - Oxymorphone
-
C: Opiod
U: Analgesic
M: MU, KAPPA, DELTA receptor agonist to block nociception
SE:dependence, constipation, nausea, vomiting, cough suppression, sedation, reduced urinary flow (and UTI)
OD: respiratory depression, coma, MIOSIS - Propoxyphene
-
C: Opiod
U: Analgesic
M: MU, KAPPA, DELTA receptor agonist to block nociception
SE:dependence, constipation, nausea, vomiting, cough suppression, sedation, reduced urinary flow (and UTI)
OD: respiratory depression, coma, MIOSIS - Tramadol
-
C: Opiod
U: Analgesic
M: MU, KAPPA, DELTA receptor agonist to block nociception
SE:dependence, constipation, nausea, vomiting, cough suppression, sedation, reduced urinary flow (and UTI)
OD: respiratory depression, coma, MIOSIS - Suboxone
- Combined Buprenorphine (partial opiate agonist) and Naloxone (opiate antagonist)
- Buprenorphine
-
C: partial opiate agonist
U: Analgesic (kidney stones)
OPIATE WITHDRAWAL
MU, KAPPA, DELTA receptor agonist to block nociception
SE:dependence, constipation, nausea, vomiting, cough suppression, sedation, reduced urinary flow (and UTI)
OD: respiratory depression, coma, MIOSIS - Naloxone
-
C: Opiate Antagonist
U: Acute Opiate OD
very fast onset
M: MU, KAPPA, DELTA receptor antagonist to block nociception
SE: May precipitate withdrawal, overshoot tachypnea
CONTRA: LIVER DISEASE - Naltrexone
-
C: Opiate Antagonist
U: Acute Opiate OD
very fast onset
M: MU, KAPPA, DELTA receptor agonist to block nociception
SE: May precipitate withdrawal, overshoot tachypnea - Clonidine
-
A-2 receptor agonist
OPIATE WITHDRAWAL RELIEF
SE: dry mouth, sedation, sexual dysfxn - 4-Aminopyridine
-
C: NMJ Block Reverser
U: Reversal of paralysis
M: Blocks K+ channels in presynaptic nerve --> allows Ca2+ channels to remain open --> increased release of ACh - Botulinum Toxin
-
C: Spamolytic
U: paralysis; removal of wrinkles
M: inhibits ACh vesicle fusion and release via cleavage of fusion protein - Hemocholinium
-
C: NMJ Blocker
U: Tx for muscle spasms
M: Blocks reuptake of choline in presynapse --> depletion of ACh stores - Succinylcholine (SC)
-
C: Depolarizing NM blocker
U: Muscle relaxation and paralysis
FAST ONSET, ShORT DURATION
M: Phase 1: slowly and reversibly binds to prejxnla nicotinic receptor --> prolonged depolarization --> inactivation of time-dependent Na channels (V-dependent still activated)
Also effector on muscarinic receptors but they recover more quickly than nicotinic
Phase 2: desensitization of nicotinic receptor to ACh
SE (esp w/ 2nd dose): malignant hyperthermia, K+ release (^ arrhythmias by keeping IMMATURE nicotinic receptors open longer) (esp burn/trauma pts), hypotension, increased IO pressue, gastic pressue, muscle pain
CONTRA: newborns, burn victims, kidney problems - Aminogycosides
-
^ NM block
(i.e. in MG effects)
-channel blocker - Dibucaine
- assesses plasma cholinesterase activity
- Magnesium
-
^ NM block
used in PRECLAMPSIA - Propoful
-
IV anesthetic
LEAST POSTOP NASEA & VOMITTING - Which 2 Non-depolarizing NM Blockers have minimal heart problems?
- Vecuronium & Cisatracurium
- St John's Wort
-
C: Herbal OTC
U: Depression
SE: INDUCES CYP450 (^ drug interaction) - Anticholinergics in Parkinsons Treatment are used in what population?
-
young patients
causes dementia in old patients - Amantidine special use?
-
Parkinson's
Antiviral agent that also blocks glutamate receptors - Curare (Detubocurarine)
-
C: Non-depolarizing NM Blocker
U: Muscle relaxation and paralysis
M: compeitive nicotinic ACh receptor antagonist. Prevents depolarization of muscle cell
SE: histamine release --> flushing, edema, erythema, HYPOTENSION, tachycardia - Mivacurium
-
C: Non-depolarizing NM Blocker
U: Muscle relaxation and paralysis
M: compeitive nicotinic ACh receptor antagonist. Prevents depolarization of muscle cell
SE: histamine release --> flushing, edema, erythema, HYPOTENSION, tachycardia - Atracurium
-
C: Non-depolarizing NM Blocker
U: Muscle relaxation and paralysis
M: compeitive nicotinic ACh receptor antagonist. Prevents depolarization of muscle cell
SE: histamine release --> flushing, edema, erythema, HYPOTENSION, tachycardia
its metabolite, Laudanosine, can cross BBB and cause seizures
^ MAC - Pancuronium
-
C: Non-depolarizing NM Blocker
U: Muscle relaxation and paralysis
M: compeitive nicotinic ACh receptor antagonist. Prevents depolarization of muscle cell
SE: histamine release --> flushing, edema, erythema, HYPOTENSION, tachycardia
Also blocks vagal tone, produces achycardia & ^ NE release
CONTRA: patient with coronary heart dz - Vecuronium
-
C: Non-depolarizing NM Blocker
U: Muscle relaxation and paralysis
M: compeitive nicotinic ACh receptor antagonist. Prevents depolarization of muscle cell
SE: VERY LITTLE histamine release (less heart problems)--> flushing, edema, erythema, HYPOTENSION, tachycardia
CONTRA: pts w/ renal failure - Cisatracurium
-
C: Non-depolarizing NM Blocker
U: Muscle relaxation and paralysis
M: compeitive nicotinic ACh receptor antagonist. Prevents depolarization of muscle cell
SE: VERY LITTLE histamine release (less heart problems)--> flushing, edema, erythema, HYPOTENSION, tachycardia
derivative of atracurium (less laudanosine, therefore less toxic) - Rocuronium
-
C: Non-depolarizing NM Blocker
U: Muscle relaxation and paralysis
M: compeitive nicotinic ACh receptor antagonist. Prevents depolarization of muscle cell
SE: histamine release --> flushing, edema, erythema, HYPOTENSION, tachycardia - -curonium & -curnium
- non-depolarizing NM blockers (i.e. curare)
- Dantrolene
-
C: central muscle relaxant
U: Anti-spasm for muscles
Baclofen = antispasm for CNS
M: inhibits Ca2+ release from SR of muscle cells, preventing contraction - Desipramine
-
C: TCA (secondary)
U: depression
M: inhibition of 5-HT and NE reuptake transporters
PARTICULARLY NE!
SE: heart block, tachycardia, ANTICHOLINERGIC EFFECTS, sedatoin, blurred vision, constipation, weight gain, orthostatic HT
OD: coma w/shock, resp depression, delirium, HT, arrhythmia - Nortiptyline
-
C: TCA (secondary)
U: depression
M: inhibition of 5-HT and NE reuptake transporters
SE: heart block, tachycardia, ANTICHOLINERGIC EFFECTS, sedatoin, blurred vision, constipation, weight gain, orthostatic HT
OD: coma w/shock, resp depression, delirium, HT, arrhythmia - Protriptyline
-
C: TCA (secondary)
U: depression
M: inhibition of 5-HT and NE reuptake transporters
SE: heart block, tachycardia, ANTICHOLINERGIC EFFECTS, sedatoin, blurred vision, constipation, weight gain, orthostatic HT
OD: coma w/shock, resp depression, delirium, HT, arrhythmia - Clomipramine
-
C: TCA (tertiary)
U: depression
M: inhibition of 5-HT and NE reuptake transporters
PARTICULARLY 5-HT
SE: heart block, tachycardia, ANTICHOLINERGIC EFFECTS, sedatoin, blurred vision, constipation, weight gain, orthostatic HT
OD: coma w/shock, resp depression, delirium, HT, arrhythmia - Amitriptyline
-
C: TCA (tertiary)
U: depression
M: inhibition of 5-HT and NE reuptake transporters
5-HT = NE
SE: heart block, tachycardia, ANTICHOLINERGIC EFFECTS, sedatoin, blurred vision, constipation, weight gain, orthostatic HT
OD: coma w/shock, resp depression, delirium, HT, arrhythmia - Imipramine
-
C: TCA (tertiary)
U: depression
M: inhibition of 5-HT and NE reuptake transporters
SE: heart block, tachycardia, ANTICHOLINERGIC EFFECTS, sedatoin, blurred vision, constipation, weight gain, orthostatic HT
OD: coma w/shock, resp depression, delirium, HT, arrhythmia - Phenelzine
-
C: MAO-A Inhibitor
IRREVERSIBLE
U: depression
M: inhibi MAO from degrading unvesicled monoamines (5-HT & NE) intracellularly
SE: hepatotoxicity, TYRAMINE TOXICITY (HT crisis)
OD: agistation, delirium, mania; seizures, hyperthermia, HT - Tranylcypromine
-
C: MAO-A Inhibitor
REVERSIBLE
U: depression
M: inhibi MAO from degrading unvesicled monoamines (5-HT & NE) intracellularly
SE: hepatotoxicity, TYRAMINE TOXICITY (HT crisis)
OD: agistation, delirium, mania; seizures, hyperthermia, HT - Trazodone
-
C: Atypical Antidepressant
U: depression
M; inhibits 5-HT reuptake adn blocks postsynaptic 5-HT2 (enhanced 5-HT1 mediated transmission)
SE: SEDATION (many use for sleep instead), dizziness, nausea
less liver toxicity - Nefazodone
-
C: Atypical Antidepressant
U: depression
M: inhibits 5-HT reuptake adn blocks postsynaptic 5-HT2 (enhanced 5-HT1 mediated transmission)
SE: SEDATION, dizziness, nausea
LIVER TOXICITY --> puled form market - Mirtazapine
-
C: Atypical Antidepressant
U: depression
SE: SEDATION
M: blocks postsynaptic 5-HT2 & A2 receptors - Buproprion
-
C: Atypical Antidepressant
U: depression
M: DA & NE reuptake inhibtion
SE: insomnia, HA, nervousness, constipation, dry moth, SEIZURES, psychosis; INHIBITS CYP450
NARROW TI
CONTRA: anorexia, bulemia, epilepsy - Carbamazepine
-
C: Anti-Seizure
U: Partial seizures, sometimes
generalized seizures
Bipolar Disorder
M: Voltage gated Na+ channel blocker
SE: diplopia, ataxia, rash, LEUKOPENIA, INDUCES CYP450
SPEEDS ITS OWN METABOLISM (have to increase dose) - Oxcarbazepine
-
Designed for those allergic to carbamzepine
SE: HYPONATREMIA - Lamotrigine
-
C: Anti-Seizure
U: Partial seizures
Bipolar Disorder
M: Voltage gated Na+ channel blocker
SE: rash, STEVENS-JOHNSONS SYNDROME, somnolence
if taken during 1st trimester, ^ chance of cleft lip or cleft palate - Phenytoin
-
C: Anti-Seizure
ADJUNCTIVE THERAPY
U: Partial seizures
Generalized seizures
STATUS EPILIPTUCUS (2nd line, given after benzo)
M: Voltage gated Na+ channel blocker
SE: Nystagmus, diplopia, ataxia, TERATOGENIC, STEVENS JOHNSONS SYN, hirsutism, GINGIVAL HYPERPLASIA, folic acid depletion, INDUCES CYP450
-need good peripheral IV or else might lose limb
-stop enteral feeds - Topiramate
-
C: Anti-Seizure
U: Partial seizures
TONIC CLONIC SEIZURES (generalized)
also treats LENNOX-GASTAUT SYN
M: Voltage gated Na+ channel blocker
Also blocks glutamate AMPA receptor; ^ GABA receptor activity
SE: slowed speech, kidney stones, aesthesia, blurred vision 2ary to glaucoma, TERATOGENIC - Zonisamide
-
C: Anti-Seizure
U: Partial seizures
M: Voltage gated Ca2+ channel blocker
SE: Irritability, anorexia - What are good drugs for generalized seizures?
-
1)Barbituates
2)Felbamate
3)Valproate
4)Phenyltoin - Ethosuximide
-
C: Anti-Seizure
U: ABSENCE SEIZURES (1st line!)
M: Voltage gated Ca2+ channel blocker
SE: dose related GI, hyperactivity, dizziness, headache - Valproate
-
C: Anti-Seizure
U: GENERALIZED SEIZURES
DOC for MYOCLONIC SEIZURES
also partial and absence seizures (2nd line)
M: Voltage gated Ca2+ AND Na+ channel blocker
SE: lethargy, tremore, HEPATOTOXICITY, weight gain, alopecia
"Fat,slow Val started losing his hair"..."and now has liver disease (hepatoxicity)" - Drugs for Status epilepticus tx?
-
1) Bezodiazepines:
LORAZEPAM
DIAZEPAM
2)Phenytoin
3)Phenobarbital (esp for INFANTS) - Viagabatrin
-
C: Anti-Seizure
U: Partial seizures
M: GABA aminotransferase blocker
SE: visual problems - Gabapentin
-
C: Anti-Seizure
U: Partial seizures
M: GABA aminotransferase blocker
SE: leukopenia - Tiagabine
-
C: Anti-Seizure
U: Partial seizures
M: GABA reuptake transporter blocker
SE: dizziness, somnolence - Selegiline
-
C: MAO-B Inhibitor
U: PARKINSONS
M: Inhibit MAO from degrade DA
SE: Tyramine txoicity
CONTRA: cheese, wine --> hypertensive episode - Rasagiline
-
C: MAO-B Inhibitor
U: PARKINSONS
M: Inhibit MAO from degrade DA
SE: Tyramine txoicity
CONTRA: cheese, wine --> hypertensive episode - Tolcapone
-
Parkinsons
COMT Inhibitor
-more LIVER FAILURE (no longer used) - Entacapone
-
Parkinsons
COMT Inhibitor
-less LIVER FAILURE - Levodopa
-
Parkinsons
SE: Vomiting, may exacerbate sym in physchotic patients b/c ^ DA - Carbidopa
-
Parkinsons
Dopa decarboxylase Inhibitor - Who are anticholinergic Parkinson's treatments reserved for?
- Young patients (old patients = dementia)
- What antiviral drug may be used to treat Parkinson's?
-
Amantidine
- also blocks glutamate receptors - Sinemet is a combination of what 2 drugs? Use?
-
Levodopa & Carbidopa
-prevents nasea - Stalevo
-
3x Combo Parkinson's Drug
Levodopa, Carbidopa & COMT Inhibitor - Bromocriptine
-
Ergoline DA agonist - DIFFUSE (all receptors)
Parkinson's & Prolactic excess
SE: fibrosis, heart valve problems, hallucinations, sedation, compulsive behavior - Pergolide
-
Ergoline DA agonist - DIFFUSE (all receptors)
Parkinson's & Prolactic excess
SE: fibrosis, heart valve problems, hallucinations, sedation, compulsive behavior - Pramipexole
-
Non-Ergoline DA agonist - D2 SPECIFIC
Parkinson's & Prolactic excess
SE: Hallucinations, sedation, compulsive behavior - Ropinirole
-
Non-Ergoline DA agonist - D2 SPECIFIC
Parkinson's & Prolactic excess
SE: Hallucinations, sedation, compulsive behavior - What other 2 additional benefits do DA agonists provide in Parkinson's Tx?
-
1) v Dyskinesia
2) Neuroprotective - What is Lithiums Mech?
-
Inhibits a-1 adrenergic receptor by INHIBITING PHOSPHATASE that creates inositol from IP3
Also ANTITHYROID for hyperthyroidism
-this prevents PIP2 from being regenerated
-also INHIBITS RELEASE of T3 and T4 from thyroid - Chlorpromazine
-
1st Generation Antipsychotic
-Temperature dysregulation - Perphenazine
- 1st Generation Antipsychotic
- Trifluoperazine
- 1st Generation Antipsychotic
- Thiothixene
- 1st Generation Antipsychotic
- Haloperidol
- 1st Generation Antipsychotic
-
Clozapine
SE? -
2nd Generation Antipsychotic
AGRANULOCYTOSIS
-therefore not used much - Risperidone
- 2nd Generation Antipsychotic
- Olanzepine
- 2nd Generation Antipsychotic
- Queiapine
- 2nd Generation Antipsychotic
- Ziprasidone
-
2nd Generation Antipsychotic
METABOLIED BY ALDEHYDE OXIDASE NOT CY450 like the rest! - Aripiprazole
- 2nd Generation Antipsychotic
- Symbax
-
Bipolar Combo Drug
Olanzepine (2nd Generation Antipsychotic) & Fluoxetine (Prozac)
SE: somnolence, weight gain - What would you use for antipsychotic drug overdose?
-
1)Bromocriptine (lecture)
2)Dantrolene (Book)