Term
| Ligand-gated ion channels |
|
Definition
|
|
Term
| G-protein Couples receptors |
|
Definition
|
|
Term
| Ionotropic glutamate receptors |
|
Definition
non-NMDA
cation Channels
AMPA
Kainate |
|
|
Term
| Metabotropic glutamate receptors |
|
Definition
| mGluR 1-8- no drugs currently target these receptors |
|
|
Term
|
Definition
| GABAb receptor agonist- inhibitory |
|
|
Term
|
Definition
ionotropic receptors for Na channels
Excitatory action in muscles and neuronal |
|
|
Term
|
Definition
Metabotropic receptors
M1, M3, and M5 are all excitatory
M2, and M4 are inhibitory
found in parasympathetic, smooth muscle, heart, CNS, and eye |
|
|
Term
|
Definition
inhibit cholinesterases- used for alzheimer
muscarinic and nicotinic agonist used for glaucoma |
|
|
Term
|
Definition
| Used for parkinson's disease |
|
|
Term
|
Definition
| Used for muscle relaxants |
|
|
Term
M1 antagonist
(scopolamine) |
|
Definition
|
|
Term
|
Definition
Mainly inhibitory, but sometimes excitatory
Broken down by COMT and MAO |
|
|
Term
| Adrenergic (Metabotropic) alpha 1 receptor |
|
Definition
| causes vasoconstriction, contraction of genitourinary smooth muscle and relaxes GI muscles |
|
|
Term
| Adrenergic (Metabotropic) alpha 2 receptor |
|
Definition
| causes platelet aggregation, inhibition of NT release, and contraction of smooth muscle |
|
|
Term
| Adrenergic (Metabotropic) Beta 1-3 receptor |
|
Definition
B1 causes increase cardiac rate and force
B2 causes broncho and vasodilation
B3 causes lipolysis |
|
|
Term
| alpha-adrenoceptor antagonist |
|
Definition
used for severe hypertension, benign prostatic hypertrophy
phaeochromocytoma |
|
|
Term
| beta-adrenoreceptor antagonist |
|
Definition
| used for Angina, MI, heart failure, HTN, glucamoa, anxiety, migraine, benign essential tremor |
|
|
Term
| alpha adrenoreceptor agonist |
|
Definition
| used for nasal congestion and BP lowering |
|
|
Term
| beta-adrenoreceptor agonist |
|
Definition
used for treatment of asthma
(salmeterol, albuterol) |
|
|
Term
| inhibitors of NE re-uptake |
|
Definition
| tricyclic antidepressants and cocaine |
|
|
Term
|
Definition
|
|
Term
| affecting NE release and storage |
|
Definition
|
|
Term
| inhibiting catecholamine metabolism |
|
Definition
|
|
Term
| Dopamine D1 and D5 receptors |
|
Definition
| excitatory receptors that activate adenyl cyclase |
|
|
Term
| Dopamine D2, D3, and D4 receptors |
|
Definition
| inhibitory receptors that inhibit adenyl cyclase and suppress Ca and activate K channels |
|
|
Term
|
Definition
molecular weight <500
LogP<5
<5 H-bond donors (NH and OH)
<10 H-bond acceptors (N and O)
<10 rotatable bonds |
|
|
Term
| Tricyclic Antidepressants(TCA) |
|
Definition
Inhibit NE and 5HT reuptake
Much less effect on dopamine, so it has little potential for abuse
Has M1, H1 and alpha 1 antagonist properties too
ADR- urinary retention, ataxia, increase Body temp, tachycardia, constipation, blurred vision, dry mouth, drowsiness, low perspiration, BP drop, weight gain and can cause sexual dysfunction
Never combine with MAOI |
|
|
Term
|
Definition
maprotilin
desipramine- 2ndary
protriptyline- 2ndary
nortriptyline- 2ndary
These are more effective in treating loss of motivation |
|
|
Term
|
Definition
Amitriptyline
Imipramine
Clomipramine |
|
|
Term
|
Definition
Fluocetine
Venlafaxine
Praoxetine
Fluvoxamine
Sertaline
Citalopram
these help treat misery and pessimism |
|
|
Term
|
Definition
inhibit 5HT > NE reuptake
mood stabilizing |
|
|
Term
|
Definition
inhibit NE > 5HT reuptake
more activating (motivation) |
|
|
Term
| Monoamine Oxidase Inhibitors (MAOIs) |
|
Definition
inhibit MAO, the breakdown of NT.
Mainly inhibit MAO-A causing more of an increase of 5HT=NE>DA
ADR- Headache, excitement, convulsions, orthostatic hypoTN, increase appetite, weight gain, constipation, dry mouth, and liver toxicity
Never combine with TCA or tyramine or food with tyramine |
|
|
Term
Fluoxetine Fluvoxamine
Sertraline Citalopram
Paroxetine S-citalopram |
|
Definition
SSRIs
more selective for SERT
should not be used for everyday tools to improve mood
used for depression (drug of choice), anxiety, OCD, and PTSD
ADR- serotonin syndrome, agitation, restlessness, rapid muscle movements, N/V, increase bowel motility diarrhea, hyponatremia and sexual dysfunction |
|
|
Term
|
Definition
SSRI
high dose can decrease weight and appetite
energizes and reduces fatigue |
|
|
Term
|
Definition
SSRI
improves energy and motivation, inhibits CYP 2D6
Can treat depression and anxiety
Sigma 1 agonist |
|
|
Term
|
Definition
SSRI
inhibits CYP 2D6
Blocks NOS which can cause sexual dysfunction
withdrawl reactions such as GI upset, restlessness, dizziness |
|
|
Term
|
Definition
SSRI
used more for OCD and anxiety. Can be helpful in psychotic and delusional depression |
|
|
Term
|
Definition
SSRI
has an R and S enantiomer. S is active against SERT.
one of the better tolerated SSRIs
inhibits CYP 2D6 |
|
|
Term
| S-Citalopram (Escitalopram) |
|
Definition
SSRI
Pure active S enatiomer
best tolerated SSRI with few CYP interaction |
|
|
Term
|
Definition
SNRI
blocks 5HT and NE uptake
Substrate for 2D6
ADR- nausea and sexual dysfunction |
|
|
Term
|
Definition
NDRI- norepinephrin dopamine
weak inhibitor of NET and DAT. The metabolites are more potent inhibitors and are concentrated in brain
can be used as anti-smoking drug
metabolized by CYP 2D6 |
|
|
Term
|
Definition
SSNRI
blocks 5-HT and NE uptake
CYP 2D6 inhibitor
can be used for depression and chronic pain |
|
|
Term
Viloxazine (Vivalan)
Atomoxetine (strattera) |
|
Definition
NRI
Atomoxetine is not approved for depression but does have therapeutic effect |
|
|
Term
|
Definition
combination of SERT inhibition and 5HT2A and 2C blockage (antagonist)
exact MOA is a ? |
|
|
Term
|
Definition
Novel 'atypical' antidepressants
MOA is a ?
sedative antidepressant that is a 5HT transport inhibitor.
substrate of CYP 3A4 |
|
|
Term
|
Definition
NaSSA- noradrenergi-specific serotonergic antidepressant
alpha 2 antagonist, increases NE, antagonist for H1, 5HT2 and 5HT3
ADR- weight gain |
|
|
Term
|
Definition
SSRi with 5HT1a partial agonist
improves mood within a week
no sexual functioning and no weight gain |
|
|
Term
|
Definition
Classic anti-epileptic
slow recovery of Na Channels from inactivation
used for partial and tonic-clonic seizures
half life increases with dose increase and disproportionately drug concentration increase
induces CYP, can hurt oral contraceptives
ADR- CNS depression, gingical hyperplasia, osteomalacia, inhibits antidiuretic hormone and insulin, tertaogenic |
|
|
Term
| Carbamazepine (Tergretol) |
|
Definition
Classic anti-epileptic
Slows Na channel recovery
used in partial and tonic-clonic seizures
metabolized to active metabolite
induces CYP 2C, 3A and UGT 9Effect PO contraceptives
ADR- stupor, coma, drowsiness, vertigo, increase in seizure frequency, N/V, skin reactions, water retention and teratogenic |
|
|
Term
|
Definition
Classic anti-epileptic
blocks t-type Ca channels in thalamus
used in absence seizures
ADR- N/V. anorexia, drowsiness, lethargy, headache |
|
|
Term
|
Definition
Classic anti-epileptic
inhibits Na, Ca channels and enhances GABA transmission by stimulate synthesis and inhibits metabolism
used in partial, generalized, absence and myoclonic seizures. (used for inclassified forms of seizures)
inhibits CYP2C9 and UGT
ADR- N/V, anorexia, eight gain, hair loss, tremor, pancreatitis, hepatotoxicity, minimal sedation, teratogenic |
|
|
Term
| Oxcarbazepine (Trileptal) |
|
Definition
New Anti-epileptic
Blocks Na channels and is a prodrug
induces 3A4/5 but inhibits 2C19. decreases PO contraceptives
ADR- dizziness, Heahache, diarrhea, N/V constipation, ataxia and nervousness |
|
|
Term
|
Definition
New Anti-epileptic
Promotes GABA release at synapse
2nd line for partial seizures. can be used for neuropathic pain, migraine and spasticity |
|
|
Term
|
Definition
New Anti-epileptic
inhibits Na channel recovery
used for partial, absence and generalized tonic-clonic seizures.
monotherapy and add on
ADR- dizziness, Blurred or double vision, N/V, and rash
risk for oral cleft for fetus. teratogenic |
|
|
Term
|
Definition
New Anti-epileptic
AMPA/kainate glutamate antagonist
blocks Na channels
activates hyper-polarizing K channels
monotherapy (>10y/o) and add on (2y/o) for partial or primary generalized seizures
ADR- cognitive impairment, somnolence, fatigue, weight loss, kidney stones teratogenic |
|
|
Term
|
Definition
New Anti-epileptic
MOA unknown
used for myoclonic, partial onset, and tonic-clonic seizures (> 4y/o)
ADR- sedation, fatigue, agitation, irritability and somnolence in kids |
|
|
Term
|
Definition
New Anti-epileptic
blocks Na and t-type Ca channels
used for add on for partial seizures
ADR- somnolence, ataxia, anorexia, kidney stones, reversible renal dysfunction, allergies with sulfonamides |
|
|
Term
|
Definition
| decrease activity, moderates excitement and calms the recipient |
|
|
Term
|
Definition
| produce drowsiness and facilitates the onset and maintenance of a state of sleep that resembles natural sleep and from which the patient can be easily roused. they are not good analgesics |
|
|
Term
|
Definition
allosteric activators of GABAa receptors. they bind to subunits alph 1,2,3 and 5. do not bind to alpha 4 and 6.
do not effect motor coordination and balance.
Do not directly open the GABAa receptor. Combo of benzo's and alcohol is lethal.
Reduce anxiety, agression, muscle tone, cause sedation, anticonvulsants, anterograde amnesia and paradoxical effects in elderly
ADRs- daytime sedation, reduction of reaction time, ataxia, falls, addictive properties |
|
|
Term
|
Definition
Antidote for overdose of benzodiazepines.
competitive inhibitor of benzodiazepines. |
|
|
Term
|
Definition
Benzodiazepines
short half life and rapid onset.
used for hypnotic |
|
|
Term
|
Definition
Benzodiazepines
short half life and slow onset.
used for hypnotic |
|
|
Term
|
Definition
Benzodiazepines
intermed half life and onset.
used for anxiolytic and hypnotic |
|
|
Term
|
Definition
Benzodiazepines
intermed half life and slow onset.
used for anxiolytic and hypnotic |
|
|
Term
|
Definition
Benzodiazepines
intermediate half life and onset
used for anxiolytic and antidepressant |
|
|
Term
|
Definition
Benzodiazepines
long half life and rapid onset
used for anxiolytic and muscle relaxant |
|
|
Term
|
Definition
Benzodiazepines
long half life and rapid onset.
used for anticonvulsant and anxiolytic |
|
|
Term
|
Definition
non-Benzodiazepines hypnotic
more selective for the alpha 1 unit on GABAa
short onset and half life |
|
|
Term
|
Definition
Z drugs- more selective for the alpha 1 unit on GABAa
Used for sedation, anticonvulsant and amnesic actions |
|
|
Term
Methohexital (brecital)
Thipental (pentothal)
Amobarbital (amytal)
pentobarbital (nembutal)
secobarbital (seconal)
phenobarbital (luminal) |
|
Definition
Barbiturates
used for anti-convulsants |
|
|
Term
|
Definition
Allosteric modulator of GABAa receptors. increase duration of channel opening.
high doses can open channel directly, which can be lethal.
induce CYPs and lots of drug-drug interactions
Not often used anymore
used for strong sedation, anticonvulsants, sleep inducing, induce respiratory and cardiovascular depression |
|
|
Term
|
Definition
melatonin MT1 and 2 receptor agnoist, this induces sleep
metabolized by CYP1A2, and is induced in smokers |
|
|
Term
|
Definition
D2 antagonist. also H1, M1 and alpha 1 antagonist. No addictive properties
improve positive symptoms but not negative and cognitive symptoms
ADR- can cause EPS symptoms, increase prolactin levels and antiemetic effect (N/V), hyslipidemia, DM, dermatological reactions, ophtahalmologic problems, urinary retention and sexual dysfunction |
|
|
Term
| Histamine H1 receptor blocker |
|
Definition
| ADR- weight gain and drowsiness |
|
|
Term
| antimuscarinic/anticholinergic (M1) receptor blocker |
|
Definition
| ADR- constipation, blurred vision, dry mouth, drowsiness |
|
|
Term
| Antiadrenergic (alpha1) receptor blockers |
|
Definition
| ADR- dizziness, drowsiness, and decreased blood pressure |
|
|
Term
| Chlorpromazine (thorazine) |
|
Definition
Classic, 1st gen antipsychotics
low D2 antagonist, high H1, M1, alpha 1 antagonist
ADR- sedation, weight gain, constipation, dry mouth, hypoTN, EPS and increase prolactin |
|
|
Term
|
Definition
Classic, 1st gen antipsychotics
Low D2 blocker, M1 antagonist
ADR- blocks K channels, possible arrhythmias, sudden death, and cardiac death.
This drug has been D/C'd |
|
|
Term
|
Definition
Classic, 1st gen antipsychotics
high D2 antagonist, moderate sedation, M1 and hypotensive effects
ADR- EPS, prolactin, sedation and hypoTN |
|
|
Term
|
Definition
Classic, 1st gen antipsychotics
High D1 antagonist, M1 antagonist
ADR- EPS, prolactin, sedative, hypoTN |
|
|
Term
|
Definition
Classic, 1st gen antipsychotics
D1 antagonist
ADR- EPS and increase prolactin release, sedation, constipation, dry mouth, hypoTN |
|
|
Term
| atypical 2nd generation antipsychotic |
|
Definition
weaker D2 antagonism and strong 5HT antagonism
can improve negative and positive symptoms. maybe used for cognitive symptoms.
less EPS and prolactin release |
|
|
Term
|
Definition
atypical 2nd generation antipsychotic
D2, 5HT, H1, alpha 1 and MY antagonist
ADR- hematotoxicity, increased seizure risk, myocarditis, weight gain and metabolic syndrome |
|
|
Term
|
Definition
atypical 2nd generation antipsychotic
high 5HT, D2 antagonist. some H1 antagonist. effective for positive symptoms
ADR- hypoTN, sedation, muscle pain, arrhythmias, long QT, and increase prolactin |
|
|
Term
|
Definition
atypical 2nd generation antipsychotic
D2 antagonist, 5HT antagonist, M1, H1, and alpha 1 antagonist
ADR-drowsiness, dizzines, weight gain, increased appetite, dry mouth and constipation
can be used for bipolar disorder |
|
|
Term
|
Definition
atypical 2nd generation antipsychotic
is a partial 5HT antagonist and agonist
short half life, weight gain, sedation |
|
|
Term
|
Definition
atypical 2nd generation antipsychotic
D2 antagonist, 5HT2a antagonist, 5HT1a agonist
ADR- little EPS, weight gain sedation and metabolic syndrom
long half life |
|
|
Term
|
Definition
atypical 2nd generation antipsychotic
partial 5HT antagonist and agonist
low EPS, prolactin increase, weight gain, dyslipidemia and insulin resistance |
|
|
Term
olanzapine
risperidone
ziprasidone
quetiapine |
|
Definition
atypical 2nd generation antipsychotic
helps with cognitive improvement
ADR- sedation, increased appetite, weight gain, metabolic syndrome, QT prolongation |
|
|
Term
|
Definition
atypical 2nd generation antipsychotic
D2 and 5HT2A antagonist
ADR- dizziness, dry mouth, fatigue, nasal congestion, orthostatic HTN, weight gain and QT prolongation |
|
|
Term
|
Definition
atypical 2nd generation antipsychotic
sub-lingual tablets
antagonist for 5HT, D2, H1, alpha 1. no muscarinic activity
ADR- risk of death, QT prolongation, EPS, release of prolactin, increased seizure threshold |
|
|
Term
|
Definition
most effective for Parkinson symptoms
pro-drug
transported into the brain by LAT and then made into dopamine
ADR- nausea, dyskinesias, hallucination, postural hypoTN, and wearing off fluctuations |
|
|
Term
|
Definition
| decarboxylase inhibitor- inhibits peripheral metabolism of L-dopa to dopamine |
|
|
Term
|
Definition
|
|
Term
|
Definition
| decarboxylase inhibitor- inhibits peripheral metabolism of L-dopa to dopamine |
|
|
Term
|
Definition
COMT inhibitor- selective and reversiblly inhibits COMT peripherally and centrally
ADR- jaundice, upset stomach, extreme tiredness, hepatotoxicity |
|
|
Term
|
Definition
COMT inhibitor- Selective and reversiblly inhibits COMT peripherally
preferred over tolcapone
ADR- nausea, orthostatic hypoTN, confusion, hallucinations, urine discoloration
can be taken with selective MAO-B inhibitor but not general MAOI |
|
|
Term
| Carbidopa/L-dopa/entacapone |
|
Definition
|
|
Term
|
Definition
| deaminates 5HT epinephrine, and NE causing unwanted side effects |
|
|
Term
|
Definition
responsible for oxidative deamination of dopamine in the brain
this is the one you would prefer to inhibit.
inhibiting MAO-B is initial therapy for treating parkinson's |
|
|
Term
| Selegiline (eldepryl, emsam, Zelapar) |
|
Definition
irreversible MAO-B inhibitor
can be given with L-dopa for advanced PD
metabolites are amphetamine and methamphetamine
ADR- anxiety, insomnia, hallucinations and possible decrease in oxidative stress
drug of choice for pts under 65 and early PD monotherapy. |
|
|
Term
|
Definition
Irreversible MAO-B inhibitor
metabolites not amphetamines
monotherapy for early PD or add on to late PD |
|
|
Term
Bromocriptine Pergolide
Piribedil Pramipexole
Ropinirole Rotigotine
Apomorphine |
|
Definition
Dopamine receptor agonist
inhibits indirect pathway
used as initial therapy in young patients or adjust to L-dopa
ADR- N/V, dizziness, orthostatic hypoTN, confusion, hallucinations, daytime sleepiness, drowsiness, somnolence, |
|
|
Term
|
Definition
Dopamine agonist that is approved for monotherapy
D2 class receptor selectivity
ADR- somnolence, hallucinations, confusion, orthostatic hypoTN |
|
|
Term
|
Definition
Dopamine agonist that is approved for monotherapy
renal cleared and available as ER formulation
ADR- Nausea, somnolence, and sleepiness |
|
|
Term
|
Definition
oldest and most potent dopamine agonist
high for D4
med for D2,3,5
low D1
good for intermittent off periods
ADR- nausea, orthostatic hypoTN, somnolence, hypersexuality and skin nodule formation |
|
|
Term
|
Definition
D2 receptor agonist
transdermal patch |
|
|
Term
Benztropine (cogentin)
Trihexyphenidyl (artane) |
|
Definition
anticholinergic/antimuscarinic
in older pts it can worsen dementia and can increase plague formation and cognitive decline
ADR- dry mouth, constipation, urinary retention, sedation, confusion, delirium and hallucinations
used as initial treatment for early PD |
|
|
Term
|
Definition
antiviral that enhances DA release, inhibits its reuptake, has anticholinergic properties and blocks NMDA receptors
Used for mild PD
ADR- confusion, dizziness, hallucinations and dry mouth |
|
|
Term
|
Definition
| implanted brain stimulator to reduce symptoms of advanced parkinson's cont controlled by medication |
|
|
Term
|
Definition
Prozac
SSRI
ADR- GI side effects and bleeds, sleep distrubances, agitation, sexual dysfunction, SIADH and anorexia
inhibits 2D6 and 4A4 |
|
|
Term
|
Definition
Paxil
SSRI
ADR- GI side effects and bleeds, sleep distrubances, agitation, sexual dysfunction, SIADH and anorexia
inhibits 2D6 |
|
|
Term
|
Definition
Zoloft
SSRI
ADR- GI side effects and bleeds, sleep distrubances, agitation, sexual dysfunction, SIADH and anorexia
weak inhibitor of 2D6 |
|
|
Term
|
Definition
Selexas
SSRI
ADR- GI side effects and bleeds, sleep distrubances, agitation, sexual dysfunction, SIADH and anorexia, QT prolongation
inhibitor of 1A2 and 3A4 |
|
|
Term
|
Definition
Lexapro
SSRI
ADR- GI side effects and bleeds, sleep distrubances, agitation, sexual dysfunction, SIADH and anorexia |
|
|
Term
|
Definition
Effexor
SNRI
ADR- tachycardia, elevated BP, insomnia, tremor, sweating, dry mouth, constipation, urinary retention,serotonin symptoms and prolonged QT |
|
|
Term
|
Definition
Pristiq
active metabolite of venlafaxine
SNRI
ADR- tachycardia, elevated BP, insomnia, tremor, sweating, dry mouth, constipation, urinary retention,serotonin symptoms |
|
|
Term
|
Definition
Cymbalta
SNRI
ADR- tachycardia, elevated BP, insomnia, tremor, sweating, dry mouth, constipation, urinary retention,serotonin symptoms and Elevated LFT
inhibits 2D6 |
|
|
Term
|
Definition
Wellbutrion-depression
Zyban- smoking cessation
NDRI- NE Dopamine reuptake inhibitor
ADR- decrease seizure threshold, NE ADRs, psychotic symptoms and bad dreams
inhibits 2D6
do not use with MAOI and use cation with dopamine, NE increasers and meds that lower seizure threshold |
|
|
Term
|
Definition
Remeron
NaSSA- noradrenergic specific 5HT antidepressants
ADR- sedation, weight gain, increased cholesterol, agranulocytosis, increase in LFT
do not use with MAOIs, and caution with NE and 5HT increasers |
|
|
Term
|
Definition
Viibryd
ADR- GI upset
CYP 3A4 substrate
do not use with MAOI |
|
|
Term
|
Definition
EmSam Patch
MAOI
ADR- NE, 5HT ADRs, psychosis, bad dreams and orthostatic hypoTN
do not use with other antidepressants, 5HT and meds that increase NE and dopamine |
|
|
Term
|
Definition
| GI side effects and bleeds, sleep distrubances, agitation, sexual dysfunction |
|
|
Term
|
Definition
Fetsima
SNRI
ADR- tachycardia, elevated BP, insomnia, tremor, sweating, dry mouth, constipation, urinary retention,serotonin symptoms
Substrate of 3A4 |
|
|
Term
|
Definition
Do not use with MAOIs and can decrease HTN medication
Cation when used with other serotonergic and NE medications |
|
|
Term
|
Definition
Do not use with MAOIs
Cation when used with other serotonergic medications |
|
|
Term
|
Definition
| tachycardia elevated BP, insomnia, tremor, sweating, and anticholinergic ADRs |
|
|
Term
| Tricyclic antidepressants |
|
Definition
ADRs- NE, 5HT, anticholinergic, sedation, weight gain, orthostatic hypoTN, arrhytmias, and decrease seizure threshold
inhibits CYP 2D6
do not use with MAOIs and use cation with NE 5HT increasers |
|
|
