Psych/neuro Flashcards
Benzodiazepines *
Drugs- alprazolam (Xanax), clonazepam (klonopin), diazepam (Valium), estazolam, flurazepam, lorazepam (Ativan), midazolam, oxazepam, quazepam (doral), temazepam (restoril), Triazolam (halcyon), chlordiazepoxide (librium), clorazepate (tranxene)
Controlled substance
MOA- enhanced GABA effect
Uses- reduction in anxiety although not DOC, sedative, hypnotic, Anticonvulsants, anterograde amnesia, muscle relaxant, muscular skeletal spasms
Not recommended in pregnancy or nursing infants
Dependence!
ADE- drowsiness, confusion, ataxia, cognitive impairment, use in caution with liver patients and alcohol use patients can enhance CNS depression, avoid with opioids can cause death
Benzodiazepines antagonist *
Drugs- flumazenil
MOA- anatagonize GABA, reverse effects of benzos for toxicity or OD
IV only
Short half life may need multiple doses
ADE- seizures if benzo was used to control; or pt is taking TCAs or antipsychotic concurrently, n/v, agitation
Antidepressants for anxiety *
SSRIs like escitalopram, paroxetine
SNRIs like venlafexine or duloxetine
Alone or in combo with benzos
4-6 weeks for effects
Buspirone *
Uses- GAD
MOA- mediated by serotonin receptors and potentially dopamine-serotonin receptors
Similar efficacy as benzo but not for acute anxiety and lacks anticonvulsant and muscle relaxant properties
ADE- HA, dizziness, nervousness, nausea, lightheartedness, minimal sedative effects
Barbiturates
Drugs- amobarbital (amytal), methohexital (brevital), pentobarbital (nembutal), phenobarbital, secobarbital (seconal)
Controlled substance
MOA- GABA enhancement receptor site different from benzos, blocks glutamate receptors
Uses- anesthesia, anticonvulsant, sedative hypotonic, can cause CNS/RESPIRATORY DEPRESSION
Do not give in pregnancy/breast feeding
ADE- drowsiness, impaired concentration, mental and psychomotor impairment, CNS depression worsens with alcohol, hangover feeling
D-D- CYP450
Contraindicated in acute intermittent porphyria
do not abrupt withdrawal can cause cardiac arrest
Death can occur from OD
No reversal agent
Zolpidem (ambien) *
Uses- hypnotic agent for about 5 hrs
MOA- binds to GABA, relative selectivity as benzos but anticonvulsant or muscle relaxant properties
Controlled substance
Few withdrawal effects
ADE- HA, dizziness, anterograde amnesia, next morning impairment, sleep walking , sleep driving
D-D- CYP450
Zaleplon (sonata) *
Oral non benzo hypnotic similar to zolpidem
Fewer residual side effects on psychomotor or cognitive function
Rapid elimination
For this have difficulty falling asleep
CYP3A4 metabolite
Eszopiclone (lunesta)*
Non benzo hypnotic
Effective for insomnia for 6 months
Rapid absorption
CYP450 metabolite
ADE- anxiety, dry mouth, HA, peripheral edema, somnolence, unpleasant taste
Melatonin receptor agonist *
Drugs- ramelteon (rozerem), tasimelteon (hetlioz)
MOA- selective agonist in MT 1 and 2, for melatonin a natural circadian rhythm hormone
Minimal potential for abuse
Uses- insomnia due to difficult falling asleep, non 24 hour sleep wake disorder
ADE- increase prolactin levels, HA, abnormal dreams, increase in LFT, URI
D-D- CYP1A2 and CYP3A4 metabolite
Antihistamine *
Drugs- diphenhydramine (Benadryl), hydroxyzine, doxylamine
Uses- mild insomnia
Sedating Antidepressants *
Doxepin- TCA
Trazodone-TCA
Quetiapine- antipsychotic
Both used for insomnia
Orexin receptor antagonist *
Drug- suvorexant (belsomra), lemborexant (dayvigo)
MOAa antagonist for OX1R and 2, ore in is a neuro peptide that promote wakefulness
ADE- nacrolepsy like, sleep paralysis, cataplexy, hypnogogic and hypnopompic hallucinations, daytime sommolence, SI
D-D- CYP3A4 metabolite
SSRIs*
Drugs- citalopram (celexa), escitalopram (lexapro), fluoxetine (Prozac), fluboxamine (Luvox), paroxetine (Paxil), sertraline (zoloft)
MOA- block reuptake of serotonin leading to increased concentrations
Takes 2-12 weeks for max benefit
Uses- MDD, anxiety, OCD, panic disorder, GAD, PTSD, social anxiety, PMDD, bulimia (Prozac only)
ADE- HA, sweating, anxiety, agitations, hyponatremia, n/v/d, weakness, fatigue, sexual dysfunction, sleep disturbances, prolong QT
Use caution in children/adolescents
Withdrawal symptoms
DOC for MDD
SNRIs*
Drugs- desvenlafaxine (pristiq), duloxetine (cymbalta), levomilnacipron (fetzima), venlafexine (effexor); milnacipran (savella)
MOA- dual inhibition of serotonin and norepinephrine reuptake
Uses- pain syndromes (savella) , depression, anxiety
ADE- nausea, HA, sexual dysfunction, dizziness, insomnia, sedations, constipation, increase in BP/HR at high doses max, sweating
Withdrawal effects
Brexanolone (zulresso)
Atypical antidepressant
MOA- positive allosteric modulator if GABA
Uses -PPD
IV
ADE- excessive sedation, loss of consciousness, hypoxia
Monitoring required
Bupropion (Wellbutrin)*
Atypical antidepressant
MOA- weak dopamine and norepinephrine reuptake inhibitor
Uses- depression, smoking cessation
ADE- dry mouth, sweating, nervousness, tremor, seizures
Low instance of sexual dysfunction
Low D-D interactions
Avoid in seizure patients and those with history of anorexia or bulimia
Esketamine (spravato)
Atypical antidepressant
MOA- S enantiomer of racemic ketamine, non selective, non competitive antagonist of N methyl D aspartate
Faster acting
Uses- adjunct therapy for treatment resistant MDD, or MDD with SI or behavior
ADE- sedative- must be monitored for 2 hours post admin; n/v, dissociation, hallucinations, elevated BP
Controlled substance for misuse
Mirtazapine (remeron)*
Atypical antidepressant
MOA- enhances serotonin and norepinephrine, antibody for alpha receptors
ADE- Sedation, increased appetite, dry mouth, weight gain
Nefazodone and trazodone *
Atypical antidepressant
MOA- weak inhibitors of serotonin and norepinephrine reuptake. Antagonist of 5HT receptor
Sedating effect
D-D-CYP3A4
ADE- priaprism, hepatotoxicity, orthostatics, dizziness, nausea, dry mouth
Vilazodone (viibryd)*
Atypical antidepressant
MOA- serotonin reuptake inhibit and 5HT receptor partial agonist
D-D CYP3A4
ADE-similar to SSRIs
Withdrawal syndrome
Vortioxetine (trintellix)*
Atypical antidepressant
MOA- serotonin reuptake inhibitor inhibition, 5HT 1 agonism, 5HT 3 and 5HT7 anatagonist
ADE- nausea; constipation, sexual dysfunctions
TCAs*
Drugs- amitriptyline, amoxapine, clomipramine (anafranil), doxepin (silenor), imipramine (tofranil), maprotiline, nortriptyline (pamelor), protriptyline, trimipramine (surmontil)
MOA- inhibit norepinephrine and serotonin reuptake, affect several other receptors like 5HT2, dopamine, histamine-more side effects than SSRIs
Uses- MDD moderate to severe, panic disorders, nocturnal enuresis, migraines, chronic pain, insomnia
ADE- blurred vision, xerostomia, urinary retention; sinus tachycardia, constipation, aggregation of angle closure glaucoma, exacerbate arrhythmia, orthostatic hypotension, dizziness, sedation, weight gain, sexual dysfunction
Uses in caution in BPD - may case a switch to manic behavior
narrow therapeutic index
Monitor those with depression and suicidal ideations
Many D-D interactions
MAOIs*
Drugs- isocarboxazid (marplan), phelelzine (nardil), selegiline (emsam), tranylcypromine (parnate)
MOA- increased stores on norepinephrine, serotonin, dopamine, inhibit MOA which catalyzes oxidation delaminating of drugs and tyramine containing foods
Uses- depression, usually intolerant or unresponsive to other agents
Many D-D interactions - no SSRIs, pseudoephedrine
Food interactions - must avoid tyramine containing foods like cheese, wine, aged meats, liver, picked or smoked fish- can cause large amounts of catecholamines to release cause hypertensive crisis, arrhythmia, cardiac arrest
ADE- drowsiness, hypotension, blurred vision, dry mouth, constipation
Serotonin-dopamine antagonist *
Second generation antipsychotic
Drugs- aripiprazole, brezipiorazole, quetiapine
MOA- block serotonin and dopamine receptors
Adjunct therapy for antidepressants
Mania and BPD*
-Lithium salt- for mania and hypomania; MOA not fully understood; therapeutic index low, monitor serum concentration; ADE- HA, dry mouth, polydipsia, polyuria, polyphagia, GI distress, tremor, dizziness, fatigue, skin reactions, sedation; signs of toxicity-ataxia, slurred speech, tremors, confusion, seizures;associated with nephrogenic diabetes insipidus, monitor thyroid function; use caution in renal patients
-valproate- also anti seizure, for maniac, not effective for MDD used as secondary agent, less toxic, monitor blood levels, no liver disease, pregnancy or mitochondrial disorders, ADE/ n/d; tremor, sedation, elevated LFTs, HA, rash, low platelet
-others-
-carbamazepine/oxabarazepine- acute maniac no blood level needed, ADE- n/v, constipation, dizziness. Rash, monitor level with cabramazepine, also WBC can cause agranulocytosis
divakproex, haloperidol, chlororpromazine, atypical antipsychotic like risperidone, olanzapine, quetiapine
-lamotrigine (not acute), unknown MOA, folic acid issues try not to use in pregnancy, ADE- HA, dry mouth, rash, DRESS
First generation antipsychotics *
Drugs- chlororomazine, thioridazine (low potency), fluphenazine, haloperidol (haldol), loxapine, molindone, perphenazine, pimozide (orap), prochlorperazine (compro, procomp), thiothixene, trifluoperazine
(High potency)
MOA- competitive inhibitors of variety of receptors mainly dopamine
More like to have EPS and movement disorders
Second generation antipsychotic *
Drugs- aripiprazole (abilify), asenapine (saphiris, secuado), brexipiprazole (rexulti), cariprazine (vraylar), clozapine (clozaril), lloperidone (fanapt), lumateperone (caplyta), lurasidine (latuda), olanzapine (zyprexa), paliperidone (invega), pimavanserin (nuplazid), quetiapine (seroquel), risperidone (risperdal), ziprasidone (geodon)
MOA- blockage of both serotonin and 5HT 2 and dopamine
Lower incidence of EPS,
Uses- first line for schizophrenic, antiemetic affects, agitation and disruptive behavior in other disorders like autism, tics
ADE- EPS, TD, neuroleptic malignant syndrome, anticholinergic effects, drowsiness, sedation, gynecomastia prolong QT, higher risk for DM, HLD, weight gain
May lower seizure threshold
BBW INCREASED RISK OF MORTALITY IN ELDERLY PATIENTS WITH DEMENTIA
Methylxanthines *
Drugs- theophylline (elixophyllin), theobromine, caffeine
Tea, cola, energy drinks, chocolate, cocoa, coffee
MOA-translocation of extra cellular calcium, increased cyclic adenosine and cyclic guanosine, inhibition of phosphodiesterase and adenosine receptors
Actions- on CNS can decrease fatigue and increased mental alertness, 1.5 grams or more can product anxiety or tremors, spinal cord is stimulated at very high doses. On CV- inotropic or chronotropic effects, diuretic. In GI- avoid in peptic ulcer stimulates gastric secretions.
Uses- asthma, migraines
Tolerance and withdrawal symptoms
ADE- insomnia, anxiety, agitation, emesis and convulsions at toxic doses, lethal dose is 10 grams (100 cups of coffee), cardiac arrhythmias
Nicotine *
Drugs- nicoderm, nicorette, nicotrol
MOA- ganglion stimulation, CNS stimulant, can produce euphoria, arousal or relaxation, improve attention; increase BP, increase vasoconstriction including coronary arteries
High doses can lead to respiratory paralysis and hypotension
Uses- not therapeutic unless weaning from cigarettes
ADE- irritability, tremors, cramps, diarrhea, increased HR, BP, increased rate of drug metabolism
Addition and withdrawal
Varenicline (chantix)*
MOA- partial agonist of nicotinic receptors in CNS, less euphoric than nicotine
Uses- weaning from cigarette, adjunct therapy
Monitor for SI, vivid nightmares, mood changes
Cocaine *
Highly addictive, schedule 2
MOA- blockade of reuptake of norepinephrine, serotonin, dopamine
Potentials and prolongs CNS and peripheral actions, and pleasure system
Chronic use can deplete stores of dopamine creating craving
Death usually due to hyperthermia
When used with etoh causes cocaethylene which further causes cardiac issues
Amphetamines *
Drugs- dextroamphetamine (Dexedrine, zenzedi), lisdexamfetamine (vyvanse) methamphetamine (speed), methylenedioxymethamohetamine (MDMA)
MOA- elevation of catecholamines and neurotransmitters in space; inhibit reuptake, similar to cocaine, decreases appetite, insomnia, CNS stimulant
Uses- some are schedule1/2, ADHD, narcolepsy, appetite suppression
ADE- at high doses psychosis and convulsions can occur, insomnia, irritability, weakness, dizziness, confusion, delirium, panic, SI, amphetamine psychosis in long term abuse, dependence, arrhythmias, CHF, cardiac arrest
Methylphenidate (concerta, cotempla, daytrana, Ritalin) *
MOA- dopamine and norepinephrine transport inhibitor
Uses- ADHD
Schedule 2
ADE- abdominal pain, nausea, anorexia, insomnia, nervousness, fever, cardiac issues similar to amphetamines, increase seizures in epilepsy
Modafinil (provigil) and armodafinil (nuvigil)*
MOA- unclear, promotes more wakefulness but less psychoactive or euphoric effects
Uses- 1st line for narcolepsy
ADE- HA, nausea, nervousness, some potential for abuse and dependence
Controlled substance
Levodopa and carbidopa*
MOA- metabolic precursors of dopamine, enhanced synthesis of dopamine
Uses- PD
ADE-anorexia, nausea, vomiting, orthostatic hypotension, tachycardia, ventricle extrasystole, arrhythmia, blood dycrasias, hallucinations, abnormal involuntary movements, mood changes
D-D vitamin pyridoxine B6, MAOIs
Selegiline (eldepryl, zelapar), rasagiline (azilect), safinamide (xadago)
MOA- selectively inhibits MAO type B the metabolite of dopamine, increases dopamine levels, Amphetamine like actions
Uses- PD
ADE- hypertensive crisis. Insomnia, nausea, serotonin syndrome, HA, confusion
Catechol -o- methyltransferase inhibitors
Drugs- entacapone (comtan), opicapone (ongentys), tolcapone (tasmar)
Uses- PD
MOA- selection inhibits COMT for increased 3 I methyldopa a levodopa metabolite
ADE- similar to levodopa-diarrhea, postural hypotension, nausea, anorexia, dyskinesia, hallucinations, sleep disorders
Monitor LFTs
Dopamine receptor agonist *
Drugs- bromicriptine(parlodel), Ropinirole (requip), pranipexole (mirapex), rotigotine neupro), apomorphine (apokyn, kynmobi)
MOA- dopamine agonist, Longer DOA than levodopa, not effective for those who have not responded to levodopa
Uses- PD complicated by motor function and dyskinesia
ADE- nausea, vomiting, somnolence, postural hypotension, loss of impulse control-uncontrolled spending, increased libido, binge eating, hallucinations, mental conditions can worsen, pulmonary fibrosis (bromocriptine)
Amantadine (gocovri)*
Antiviral by nature but has PD uses
MOA- releases dopamine, blocks cholinergic receptors, inhibits NMDA
ADE- restlessness, agitation, confusion, hallucinations, high doses can induce psychosis, orthostatic hypotension, urinary retention, edema, dry mouth
Antimuscarinic drugs
Drugs- benztropine (congentin), trihexyphenidyl
Uses- PD
MOA-Blockage of cholinergic transmission, helps correct dopamine and acetylcholine balance
ADE- mood changes, confusion, zerostomia, constipation, visual problems
Adenosine receptor antagonist *
Drugs- istradefyllibe (nourianz)
MOA- antagonist for adenosine A2A receptor
Uses- PD, adjunct therapy with levodopa/carbidopa
ADE- dyskinesia, nausea, constipation; hallucinations, insomnia, loss of impulse control
Acetylcholinesterase inhibitors *
Drugs- donepezil (aricept), galantamine (razadyne), rivastigmine (exelon)
Uses- Alzheimer’s
MOA- inhibits acetlycholinesteraae which improves selectivity for acetylcholine transmission
ADE-nausea, diarrhea, vomiting, anorexia, tremors, bradycardia, muscle cramps
NMDA receptor antagonist *
Drug- memantine (namenda)
Uses- Alzheimer’s
MOA- antagonist for NMDA which is thought to accelerate apoptosis
Well tolerate some ADE include confusion, agitation and restlessness
Often used in combo with acetlychonlinesteraae
Aducanumab (aduhelm)
Class- amyloid beta directed monoclonal antibody
Uses- Alzheimer’s
MOA- reduces amyloid plaques in the brain uncertain if it delays progression
ADE- Brain edema, micro hemorrhage, HA, diarrhea
Sphingosine 1 phosphate receptor modulators
Drugs- fingolimod (gilenya), ozanimod (zeposia), ponesimod (ponvory), siponimod (mayzent)
Uses-MS
MOA-alter lymphocyte migration by modulating sphingosine 1 phosphate receptors, reduce lymphocytes in CNS
ADE- bradycardia, macular edema, PML, increased risk for OI
Teriflunomide (aubagio)
MOA- pyrimidine synthesis inhibitor and decreased lymphocytes in CNS
Uses-MS
ADE- elevated LFTs, avoid in pregnancy
Nuclear factor like 2 activators
Drugs-Dimethyl fumarate (tecfidera), diroximel fumarate (vumerity), mono methyl fumarate (bafiertam)
MOA- activated nuclear factor like 2 antioxidant pathway
Uses- MS
ADE- OI, PML, liver injury
Brivaracetam (briviact)*
Uses- treatment of focal seizures in adults
MOA- high and selective affinity for synaptic vesicle protein, exact MOA unknown
D-D CYP450
Cannabidiol (epidiolex)
Uses- seizures due to Lennox gastaut syndrome, Dravet syndrome, Tuberous sclerosis complex
MOA- canibinoid like but no psychoactive features
D-D- CYP450
ADE-drowsiness, diarrhea, vomiting, decreased appetite, elevated LFTs
Carbamazepine ((tegretol) *
Uses- also can be used for BPD, focal seizures, tonic clonic, trigeminal neuralgia
MOA- blocks sodium channels inhibiting generation of repetitive action potential
D-D- CYP1A2, CYP2C, CYP3A, UGT
ADE- hyponatremia
Do not give in absent seizures type can increase seizures
Cenobamate (xcopri)*
MOA- sodium channel blocker, Modulates GABA
Uses- focal seizures
ADE- fatigue, HA, dizziness, double vision
Eslicarbazepine (aptiom)*
MOA- sodium channel blocker
Uses- focal seizures
ADE/ dizziness, somnolence, diplopia, HA, rash, psychiatric effects, hyponatremia
Ethosuximide (zarontin)*
MOA- reduces prolongation of animal electrical activity in the brain by inhibiting T type calcium channels
Used- absent seizures
Felbamate (felbatol)
Uses- broad spectrum, reserves for refractory epilepsy like Lennox gastaut syndrome
MOA- blocking sodium channels, competing with NMDA sites, blocks calcium channels and potential GABA
ADE- aplastic anemia, hepatic failure
Fenfluramine (fintepla)
Uses- dravet syndrome related seizures
MOA- 5 HT 2 receptor agonist
ADE- valvular heart disease and pulmonary HTN, drowsiness, lethargy, reduced appetite, weight loss
Gabapentin (neurotin) *
MOA- exact unknown
Uses- many but seizures in this case
ADE- mild usually well tolerated
Few D-D interactions
Lamitrigine (lamictal)
MOA- block sodium Channel and calcium channel
Uses- focal, generalized, absent and Lennox gastaut syndrome, BPD
Slow titration
ADE- rash, to life threatening
Levetiracetam (keppra)*
Uses- treatment of focal onset seizures and adjunct for myoclonic and tonic clonic in children and adults
MOA- high affinity for synaptic vesicle protein
ADE- mood alterations lower dose to reduce
Few D-D
Oxcarbazepine (trileptal)*
MOA- reduces to 10 mono hydroxy metabolite responsible for anticonvulsant activity, blocks sodium channels and some calcium
ADE- hyponatremia
Phenobarbital and primidone (mysolin)*
Pheno-inhibitory effects of GABA, used in status epilepticus when other agents fail
Primidone- metabolizes to phenobarbital and phenylethylmalonamide both are anticonvulsant
Phenytoin (dilantin) and fosphenytoin (cerebyx) *
MOA- sodium channel blocker
Uses- focal and generalized tonic clonic, status epilepticus
ADE- CNS depression, gingival hyperplasia, long term use can cause peripheral neuropathy and osteoporosis
Fosphenytoin can be given IM and phenytoin CANNOT CAUSES TISSUE NECROSIS AND DEATH
Pregabalin (Lyrica)*
MOA- bunds to subunit of Calcium channels inhibiting excitatory neurotransmitter release
Uses- focal onset seizures, diabetic neuropathy, posttherpetic neuralgia, fibromyalgia
ADE- few
D-D- few
Rufonamide (banzel)*
MOA- sodium channel
Used- adjunct for Lennox gastaut syndrome in children 1 year or older and adults
Food increase absorption
D-D- carbamazepine and Pheytoin can decrease concentration and valproate cane increase
ADE- short QT
Stiripentol (diacomit)*
MOA- modulate GABA
Uses- dravet syndrome along with clobazam
Tiagabine (gavitril)
MOA- GABA reuptake inhibitor
Uses- adjunct for focal seizures
Topiramate (topamax)*
MOA- blocks sodium channels, reduce calcium currents and acts in NMDA site
Uses- focal seizures and primary generalized epilepsy
D-D- Pheytoin, carbamazepine
ADE- somnolence, weight loss; paresthesia, kidney stones, glaucoma l, decreased sweating, hyperthermia
Valproic acid
Valproate
Divalproex (depakote) *
MOA- sodium channel blockage and blocks GABA, and T type calcium channel
Uses- focal, primary generalized epilepsy
ADE- liver toxicity avoid in women and children under age 2
Vigabatrin (sabril)*
MOA- irreversible bind to inhibit GABA
ADE- vision loss
Not widely used
Zonisamide (zonegran)*
MOA- Sulfa derivative blocks sodium and calcium channels
Uses- focal
ADE- kidney stones, CNS issues, hyperthermia, decreased sweating
Contraindicated in sulfa allergies or carbonic anyhydrase inhibitor allergy
Actetylcholine (miochol E)
MOA- “rest and digest”, inactivates cholinesterases
-decreased HR and cardiac output, decreased blood pressure, increases salary secretion, gastric secretion, broncoconstriction, detrusor activity, constriction of pupils
Direct acting cholinergic
Bethanechol (urecholine)*
Direct acting cholinergic
MOA- rest and digest properties, muscarinic receptor activity
Uses- stimulate atonic bladder, urinary retention
ADE- sweating, salivation, flushing, decreased BP, abdominal pain, diarrhea, bronchospams
Cabachol (miostat)
Direct acting cholinergic
MOA- rest and digest action, muscarinic action
Uses- eye surgery of constriction and decrease IOP
ADE- few is used ophthalmic
Pilocarpine (salagen, isopto carpine)*
Direct acting cholinergic
MOA- rest and digest properties
Uses- glaucoma, DOC to reduce IOP emergency for open and angle closure glaucoma
ADE- blurred vision, night blindness, brow ache
Edrophonium (enlon)
indirect cholinergic
MOA- rest and digest properties, binds to acetylcholine
Uses- MG by increase amounts of acetylcholine to peripheral muscle
not DOC better agents removed from market
Physostigmine *
Indirect cholinergic agonist
MOA- rest and digest, muscarinic stimulation that causes GU smooth muscle contraction, miosis, bradycardia, hypotension
Uses- OD on anticholinergics
ADE- convulsions, decrease CO, skeletal muscle paralysis
Neostigmine (bloxiverz)*
Indirect cholinergic agonist
MOA- rest and digest properties but cannot enter CNS, and greater action on skeletal muscles and stimulates contractility
Uses- stimulate bladder and GI tract and reversal agent for paralytic agents, MG symptoms
ADE- salivation; flushing, decrease BP, nausea, abdominal pain, diarrhea, bronchospams
Contraindicated in intestinal or urinary bladder obstruction
Pyridostigmine (mestinon)*
Indirect cholinergic agonist
Uses- MG
ADE similar to neostigmine
Tacrine
Donepezil (aricept)
Rivastigmine (exelon)
Galantamine (razadyne)
Indirect cholinergic
Uses- Alzheimer’s due to deficiency in acetylcholine, delays AD progression
Atropine
Anticholinergic
MOA- prevents acetylcholine binding, fight or flight properties
Uses- eye dilation, antispasmodic for GI tract, increased HR, antidote for cholinergic OD
ADE-dry mouth, blurred vision, tachycardia, urinary retention, constipation, delirium, CNS changes
Scopolamine
Anticholinergic
MOA - blocks acetylcholine, fight or flight properties
Uses- motion sickness, sedation at high doses
ADE- same as most anticholinergics
Ipratropium (atrovent)
Anticholinergics
MOA- blocks acetylcholine, fight or flight properties
Uses- promote bronchodilation in asthma/COPD
Inhalation
Tropicamide (mydriacyl) and cyclopentolate (cyclogyl)
Anticholinergic - fight or flight properties
Ophthalmic solution for eye dilation
Benztropine (congentin) and trihexyphenidyl
anti cholinergic- fight or flight properties
Adjuvants for PD, or EPD caused by antipsychotics
Oxybutynin (ditropan, gelnique, oxytrol)
Anticholinergic- fight or flight properties
Uses- overactive bladder
ADE- dry mouth, constipation, blurred vision, fewer CNS issues
Ganglionic blockers
For smoking cessation on nicotinic receptor
Anticholinergics
Non depolarizing blockers
Drugs-tubocurarine, cisatracium (nimbex), mivacurium (mivacurium), rocuronium, vecuronium
MOA- block acetylcholine on skeletal muscles
Uses- paralyzing muscles for surgery, intubation
ADE- few
D-D- cholinesterase inhibitors, halogenated hydrocarbon anesthetics, aminoglycoside, CCB
Succinylcholine (anectine, quelicin)
Neuromuscular blocking agent
MOA- binds to nicotinic and acetylcholine receptors, mainly affects respiratory muscles
Uses- intubation
ADE- hyperthermia, prolonged muscle weakness, hyperkalemia
Epinephrine (adrenaclick, adrenalin, epipen)
Direct acting adrenergic agonist
MOA- interacts on both alpha and beta receptors. Fight or flight properties
-increase HR, CO, vasoconstriction, bronchodilator, hyperglycemia
Uses-bronchospasm, anaphylaxis, cardiac arrest, adjunct to local anesthesia
ADE-anxiety, fear, tension, HA, tremor, arrhythmia, pulmonary edema, tachycardia,
Norepinephrine (levophed)
Direct acting adrenergic agonist
MOA- alpha receptors, fight or flight not as strong as epi
-vasoconstriction, baroreceptor reflex which can trigger bradycardia, may diminish blood flow to kidneys
Uses- shock
ADE-similar to epi, blanching and sloughing of skin, tissue necrosis if extravasation occurs, give in central vein
Dopamine
Direct acting adrenergic agonist
MOA-alpha and beta receptors and dopaminergic receptors fight or flight properties
-increased CO, vasoconstrictions, increase blood flow to kidneys,
Uses- cardiogenic shock, septic shock, hypotension, CHF, bradycardia
ADE- same as other and nausea, hypertension, arrhythmias
Phenylephrine (neo synephrine, sudafed PE)
Direct acting adrenergic agonists
MOA-alpha receptor activity, fight or flight
-vasoconstriction, reflex bradycardia,
Uses- hypotension in hospitalized or surgical patients especially if tachycardia, nasal decongestant, eye dilation
ADE- hypertension HA, cardiac irregularities
Naphazoline, oxymetazoline (afrin), tetrahydrozoline (visine)
direct acting adrenergic agonist
MOA-act on alpha 1 and alpha 2 receptors
-vasoconstriction,
Uses- nasal decongestant, rosacea
ADE- nervousness, HA, trouble sleeping, irritation, sneezing
Do not use for more than 3 days due to rebound congestion
Midodrine
Direct acting adrengeric agonist
MOA- selective alpha agonist
Increases BP
Uses- orthostatic hypotension
Given 3-4 X a day
To avoid supine hypertension do not give within 4 hours of bedtime
Clonidine (catapres, duraclon)
Direct acting adrenergic agonist
MOA- acts on alpha 2 receptors, which deceased sympathetic outflow to peripheral
Uses- HTN, ADHD
ADE- lethargy, sedation, constipation, xerostomia
Abrupt DC can cause rebound HTN
Dobutamine
direct acting adrenergic agonist
MOA- beta 1 receptor and some beta 2 and alpha 1
-increase HR, CO, few vascular issues
Uses- inotropic support after cardiac surgery, acute CHF
use caution in a fib as it increases AV conductors
ADE- similar to epi
Tolerance
Isoproterenol (isuprel)
Direct acing adrenergic agonist
MOA- beta 1 and beta 2
-increases HR, CO, dilation of skeletal muscle arterioles, slight BP increase, potent bronchodilator
ADE- similar to epi and beta receptor agonist
Albuterol (proair, proventil, ventolin), levoalbuterol (xoponex), metaproterenol, terbutaline
direct acting adrenergic agonists
MOA- short acting beta 2 agonist
Uses- bronchodilator, by inhaler
Terbutaline also used to suppress premature labor
ADE- tremor, restlessness, apprehension, anxiety, tachycardia, arrhythmias,
D-D- MOAIs can potentiate CV ADE
Formoterol (foradil, perforomist) indacaterol (arcapta), olodaterol (striverdi), salmeterol (serevent)
Direct acting adrenergic agonist
MOA- beta 2 selective
Uses- asthma, COPD by inhaler like dry powder, long acting
Effective when used in combo with inhaled steroid
Mirabegron (myrbetriq) and vibegron (gemtesa)
Direct acting adrenergic agonist
MOA- act on beta 3 which relaxes Detrusor muscle and increases bladder capacity
Uses- OAB
Mirabegron may increase BP
D-D- can increase digoxin level, CYP2D6
Indirect acting adrenergic agonist
-amphetamine- alpha 1 and beta 1 activity- increased BP, increase HR
-tyramine- not a clinical drug but found in aged cheese, wine, fermented foods- if concurrently taking a MOAI can cause catecholamine release
-cocaine- blocks sodium and chloride, causing norepinephrine to remain in synapse, increases BP by alpha 1 and beta effects
Mixed action adrenergic agonists
Drugs- ephedrine (akovaz, emerphed) and pseudoephedrine (sudafed, genaphed)
MOA- act on alpha and beta receptors, similar to epinephrine, Long duration of action
-raises BP, bronchodilator, alertness, decrease fatigue, prevents sleeps
Uses- nasal decongestant
Phenoxybenzamine (dibenzyline)
Adrenergic blockers
MOA- blocks alpha 1 and alpha 2
-decreased BP, reflex tachycardia
Uses- reverse epinephrine, swearing, HTN with pheochromocytoma, off label-HTN crisis, neurogenic bladder, prostate obstruction
ADE- postural hypotension, nasal stuffiness, inhibited ejaculation, GI irritation, reflex tachycardia
Phentolamine
Adrenergic blocker
MOA- blocks alpha 1/2
Uses- for dx of pheochromocytoma and HTN crisis, can be used locally for dental procedures
Prazosin (minipress), terazosin, doxazosin (cardura)
Adrenergic blockers
MOA- alpha 1 receptor blocker
-relaxes smooth muscles, some decrease in BP
Uses- HTN but not first line, BP
Take at bedtime to avoid orthostatic hypotension
ADE- dizziness, fatigue, nasal congestion, HA, drowsiness, orthostatic hypotension, floppy Iris syndrome
Propranolol (inderal, innopran)
Adrenergic blocker
MOA- beta blocker 1 and 2 receptors
-diminishes CO, negative inotrope, bradycardia, decrease in cardiac workload, decrease BP, bronchoconstriciton, decreased glucose and glucagon
Use- angina, HTN, MI, migraine, hyperthyroid
ADE- bronchoconstriction, arrhythmias if stopped abruptly, hypoglycemia, depression, fatigue, dizziness, lethargy, weakness, visual disturbances
D-D- CYP1A2, CYP2D6- bupropion, fluoxetine, paroxetine, quindine, amiodarone, diltiazem, lidocaine
Nadalol (corgard) and timolol (betimol, istalol, timoptic)
MOA- Non selective beta antagonists
Uses- open angle glaucoma, portal HTN in cirrhosis
Acebutolol, atenolol (tenormin), betaxolol (betoptic), bisoprolol, esmolol (brevibloc), metoprolol (lopressor, toprol), nebivolol (bystolic)
MOA- Selective beta 1 antagonist, lower BP, increase exercise tolerance in angina, arrhythmia control
Uses- angina, CHF,
Acebutolol and pinodol
MOA-Antagonist but weakly stimulate beta 1/2
Uses- HTN with some bradycardia
Labetalol and carvedilol (coreg)
MOA- antagonist for alpha and beta receptors
Uses- pregnancy induced HTN, CHF, emergency anti HTN
ADE- orthostatic hypotension, dizziness
Sleep
1st like melatonin
If not Adequate can they trazadone, mirtazapine, doxepin, amitriptyline
SSRI OD
Citalopram can cause QT prolong and arrhythmias
Seizures
Serotonin syndrome- hyperthermia, muscle rigidity, sweating, myoclonus, mental status change, unstable vitals
DC syndrome *
From abrupt antidepressants withdrawal, Prozac has lowest risk for syndrome due to half life
HA, malaise, flu like syndrome, agitation, irritability, nervousness, changes in sleep
Combination therapy *
Bupropion can be added to SSRI or SNRI most common
Mirtazapine added to SSRI or SNRI-2nd line
Trazodone to SSRI SNRI- 3rd line
TCA to SSRI or SNRI- last try
MDMA aka molly aka ecstasy
Hallucinogenic properties with serotonin release
Bruxism and jaw clenching
Hyperthermia, AMS, serotonin syndrome
Cyproheptadine
Tx for serotonin syndrome
Synthetic cathinones aka bath salts
Cause catecholamine release like cocaine and amphetamines
Similar tx for cocaine or meth
LSD
Psychedelic effects potent agonist of 5HT2a receptors
Hallucinations, mood and sleep alterations, anxiety
Hyperthermia, tachycardia, HTN
Losing judgement and impaired reasoning
MJ
THC main psychoactive component
Can produce euphoria, drowsiness, relaxation
Mood hallucination effect
Withdrawal- cravings; insomnia, MDD, pain or irritability
Etoh abuse tx
Disulfiram (anatbuse( blocks oxidation of acetylhyde
Results in accumulation causes flushing, tachycardia, hyperventilation, nausea
Naltrexone- competitive and long action opioid agonist to decrease craving
Acamprosate- decrease craving by NMDA effects
Direct acting anti cholinergic
Acetylcholine- muscarinic and nicotinic receptors -decrease HR, and cardiac output, lower BP, increase gastric acid secretions and saliva production, vasoconstriction, can increase bladder tone and pupil constriction
Cevimeline (evoxac)
Direct acting cholinergic agonist
Produce secretions, less effect on BP
For xerostomia in XRT and sjorgrens
Anticonvulsants classes
Benzos
Bind synaptic vesicle protein- keppra, briviact
Sodium channel blockers/ tegretol, trileptal, aptiom
Hydantoins- Dilantin, cerebyx
CCB- zarotin
Glutamate effects- fycompa
Barbiturates- primidone; phenobarbital
GABA effects/ xcopril, diacomit, Antrim, sabril
multiple- depakote, felbatol, vinpat, lyrica, lamacital, topamax, zonegran
Unknown- epidolex, fenetepla, neurotin, banzel
