methylphenidate
ADHD tx DA and NE reuptake inhibitor -short acting 2-4 h -SANS side effects -possible effect on growth(controversial)
Adderall
ADHD
-amphetamine
only advantage over methylphenidate that it’s longer acting ( 12-14 h)
-
Atomexetine
ADHD
preferentially NE action, so no dependence potential, more effective on attention
potentially may replace methylphenidate as a drug of choice for ADHD
Pemoline
ADHD
long acting DA agonist
less efficacious and risk of fulminant hepatatis
Pramipexole
direct DA agonist
- effective as levodopa in early disease, but not in late stage
- Neuroprotective
- SE: sleep attacks,risk of OCD
Ethanol
antitremor
-effective for essential tremor
Ropinirole
Direct acting DA agonist
propranolol
antitremor
-effective for essential tremor
Benztropine
antimuscarinic and DA reuptake inhibitor (takes advantage of DA/AcH balance theory)
tx of parkinsonism effects of antipsychotics
Aripiprazole
atypical antipsychotic(Abilify) MOA: partial antagonist of D2 receptors (80% selective) very low risk of EPSA
Quetiapine
2nd geniration antipsychotic (Seroquel) MOA: partial 5HT 1A agonist DA antagonist (Not much D2) serotonin antagonist antihistamine
Low EPSA +tardive Dyskinesia
high weight gain
high sedating
high orthostasis
Dystonia drugs
antimuscarinics
benzodiazepines
botox
Trihexyphenidyl
ANTIMUSCARINIC, almost no effect on DAT
used to tx parkinsonism signs of antipsychotics
Ziprasidone
atypical antipsychotic
MOA: D2, D3, 5HT antagonist
Also 5HT1A agonist-may alleviate anxiety and depression
OLANZAPINE
2nd generation antipsychotic, atypical
MOA: D4 anatgonist, little D2(reason for atypica?)
Potent antimuscarinic
Low EPSE low TD low orthostasis high weight gain high sedating
risperidone
2nd generation antipsychotic, atypical
MOA: some DA anatgonist, potent 5HT antagonist
-Atypical ONLY at LOWER doses
Clozapine
atypical antipsychotic
MOA: D4 antagonist w/little striatal D2 anatagonist (reason for Atypical)
potent antimuscarinic
-very effective for psychosis/hallucination associated with PD meds
-very effective for negative symptoms, i=unlike other atypicals
- paradoxical wet pillow-excessive drooling
- risk of agranulocytosis
diazepam(valium)
BENZODIAZEPINES (prototypical)
96 h half life
long acting used for anxiety and problems staying asleep, as well as managemnt of seizures from alcohol withdrawal
triazolam
benzodiazepine,
for troubles falling asleep
short-acting 3-8 h.
more associated with anterograde amnesia
lorazepam(ativan)
benzodiazepine intermediate acting (10-20 h) FDA approved an antianxiety -used for status epilepticus safe for people with compromised liver function because conjugated outside liver
estazolam
benzodiazepine
intermediate acting
for longer sedation and trouble staying asleep
flumazenil
direct acting competitive benzodiazepine antagonist
-used to reverse BZD/alcohol inuced coma
pentobarbital
barbiturate
-used to induce coma in status epilepticus
phenobarbital
barbiturate
autoinducer
1/day dose, long half life
-used to manage generalized seisures
zolpidem (Ambien)
-benzodiazepine-like
does not suppress REM, little musle relaxant, little rebound insomnia
Meprobromate
anti-anxiety
greater potential for tox in overdose; SE: hypotension, respiratory arrest
Eszopiclone(Lunesta)
-benzodiazepine-like, safe for chronic use because low tolerance
Remelteon
-new type of sedative hypnotic
melatonin agonist, no adverse events but not as agood a sedative
Zeleplon
short duration sedative hypnotic for troubles falling asleep, but NOT staying asleep
Buspirone
selective anxyolytic, 5HT-1A partial agonist, small anti DA
effective for generalized anxirty, but not panic attacks
no dependence, no sedation, no anti-epileptic
Propranolol
selective anxiolytic
stage freight
baclofen
anti-spastic
GABA-B specific (only in spinal cord)
reduces afferent reflexes mediating spasticity
less sedating than BDZ in anti-spastic doses, but withdrawal effects are severe hyper-spasticity and seizures- higher doses delivered intrathecally are used
CNS depressants
anesthetics, alcohol, BDZs, barbiturates
codeine
opioid analgesic, full agonist
-converted to morphine
-less sedating and analgesic, but more antitussive (affinity for Glu receptors)
-adverse affects similar to morphine but less severe
HIGH constipation
morphine
opioid analgesic
“morphine flush”
heroine
opioid analgesic, full agonist
converted to morphine and produces “morphine flush”
-greater dependence risk than morphine because enters the brain quicker(more lipid soluble)
hydromorphone(dilaudid)
opioid analgesic, full agonist
hydrocodone (vicodin)
opioid analgesic, full agonist
-used in combinations with acetominophen and ibuprofen
analgesic and antitussive potency»codeine
oxycodone
opioid analgesic, full agonist
SUSTASINED RELEASE
often abused
meperidine(demerol)
- opioid analgesic, full agonist
- 1/10 morphine potency
- metabolite non-peredine can cause CNS excitation in patients with renal disease or in high doses
- in combination with MAOI-serotonin syndrome, because inhibits seratonin transporter
fentanyl
opioid analgesic, full agonist
80 times > morphine
NEVER to non-tolerant patients due to respiratory depression risk
methadone
opioid analgesic, full agonist
cross linking with morphine, but long acting, great oral availability, easier to withdraw from
-tx of narcotic abstinence syndrom and methadone program
propoxyphene
opioid analgesic, full agonist
pentazocine
prototypical partial opioid agonist
- respiratory depression ceiling effect
- minor withdrawal symptoms when swithced from full agonist
- psychotomimetic effect in high doses
buprenorphine
partial mu opioid agonist
similar to varenicline in smoking sessation used to treat opiod abstinence patients
naloxone
opioid antagonist
- used to treat opioid overdose(coma, miosis, respiratory depression); very short 1/2 life so pt. has to be monitored not to slip back into coma
- always IV
- can trigger withdrawal in addicts and reduce pain threshold in normal people
naltrexone
opioid antagonist
effects similar to naloxone, but used less frequently and available in ORAL form
Tramadol(ultram)
partial opioid mu agonist(analgesic)-effects not as pronounces (e.g respiratory depression
NE and 5HT reuptake inhibitor-potentiate opiod actions
dextromethorphan
non- narcotic centrally acting antitussive, Glu antagonist
antitussiv effect similar to codeine but no analgesic, euphoric or respiratory deprssion side effects
diphenoxylate with atropine
opioid like, tx of diarrhea
atropin( antimuscarinic-constipation+ unpleasant side effects when large doses)
loperamide(imodium)
opiod like; tx of diarrhea
doesn’t cross BBB, but if used with greapfruit juice -morphine like effects
Imipramine
tca
amitriptyline
TCA
trazodone
heterocyclic antidepressant, 5HT2 antagonist, Glu release, paradoxical
fluoxetine
SSRI
- very long half-life, so interaction with other antidepressants possible when switching meds, but skipped dose is not that important
- high potential of CV and CNS drug interaction
venlafaxine
5HT and NE reuptake inhibitor
phenelzine
MAOI, suicide inhibition
lithium carbonate
antimanic
carbamazepine
antimanic
valproate
antimanic
bupropion
NE and DA reuptake inhibitor
venlafaxin
SNRI
Mertazapine
NE and serotonin specific reuptake inhibitor, alpha antagonist
selegiline
Indirect DA tone agonist, selective MAO-B inhibitor
converted to amphetamine/methamphetamine-DA, NE, 5ht reuptake inhibitors that further increases DA
-tx PD symptoms and slows Clinical progression
rasagiline
Indirect DA tone agonist, selective MAO-B inhibitor
DOESN’T convert to amphetamine
tolcapone
Indirect DA agonist,peripheral and central COMT inhibitor
-cross BBB and increases levodopa availability and length of action in brain
T for TOTAL COMT inhibition and Liver TOXICITY
entacapone
Indirect DA agonist, peripheral COMT inhibitor
-extends levodopa availability to brain, does not cross BBB
ropinirole
direct DA agonist
- effective as levodopa in early disease, but not in late stage
- Neuroprotective
- SE: sleep attacks, risk of OCD
haloperidol
typical antipsychotic
highest therapeutic index
huntington’s and torret
chlorpromazine
typical antipsychotic
thioridazine
typical antipsychotic, but
doesn’t cause EPSEs due to its muscarinic activity
fluphenazine
typical antipsychotic
Apomorphine,
Syrup of epicac
Emetics,
Act on CTZ
Prochlorperazine, ondansetron, metoclopramide
Antiemetic
Act on CTZ