Drug List Psychopharm

8/13/2019 Drug List Psychopharm

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Dr. Shane Bradley

Psychopharmacology Outline Winter/Spring 2013

Drugs Used to Treat Anxiety

Benzodiazepines

Bind to type A aminobutyric acid (GABAA) receptor complex on the alpha subunit, which is known as the benzodiazepine (BZ) or

omega receptor. The GABAA complex is associated with neuronal chloride channels, and when benzodiazepines bind to their

receptors, increasing the affinity of GABA for its receptor site enhances the channel opening effect. This increases the frequency

of chloride-channel opening, creating a hyperpolarized cell membrane that prevents further excitation. From

https://secure.pharmacytimes.com/lessons/200306-01.asp

Indications/uses include anxiety d/o, panic d/o, mania, seizure d/o, phobias, insomnia, alcohol withdrawal, muscle spasm,

agitation, catatonia, akathisia, night terrors

Side effects

sedation, cognitive impairment, anterograde amnesia

respiratory depression at high doses or with alcohol

may worsen obstructive sleep apnea symptoms

disinhibition in susceptible individuals

Effect on sleep


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decrease in sleep latency, increase in sleep time, an increase in Stage 2 sleep, and a small decrease in delta and REM sleep

Diazepam- very long half life; excellent muscle relaxant

Chlordiazepoxide- very long half life; excellent for alcohol withdrawal

Clonazepam- long half life; also used in many forms of seizures

Estazolam- short to medium

Temazepam- short to medium

Oxazepam- short to medium

Alprazolam- short to medium

Lorazepam- medium

Midazolam- very short, operation pre-sedate, amnestic

Triazolam- very short

Antihistamine: Hydroxazine, very safe; side effects = anticholinergic at high doses

Diphenhydramine, very safe, side effects = anticholinergic at high doses

Unique mechanism of action: Buspirone

5-HT 1A (presynaptic) agonist. This effect decreased serotonergic tone in the dorsal raphe, which is COMPLETELY counterintuitive to what you

would expect from an anxiolytic. It also binds to dopamine type 2 (DA 2) receptors (presynaptic) as an antagonist, thereby increasing

dopaminergic tone. It also increase noradrenergic tone in the locus ceruleus.


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Considered less effective than benzodiazepines, but some studies show similar result. Considered particularly safe.

Alpha (2) adrenergic agonists

prazosin

prazosin found helpful in reducing PTSD related nightmares- evidence-based

Beta Blockers

propranolol (Inderal) is primary BB of choice in mental health.used for akathisia, lithium-induced tremor, performance

anxiety & aggressive behavior (hyperarousal) (other lipid soluble = pindolol, labetolol, metoprolol)

avoid in asthma, diabetes if patient is prone to hypoglycemia (especially if prone to hypoglycemia unawareness), bradycardia,

second or third degree heart blocks

Drugs Used to Promote Sleep

perspective: http://www.medscape.com/viewarticle/759336

Melatonin agonist:

Ramelteon Side effect note: generally safe, rare hyperprolactinemia, half life 2-5 hours/fx last 8

Specific Gaba 1A agonists
http://www.medscape.com/viewarticle/759336http://www.medscape.com/viewarticle/759336http://www.medscape.com/viewarticle/759336


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Drugs Used to Improve Mood and/or Decrease Anxiety

SSRIS

Half-life

Short:paroxetine & fluvoxamine (


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Serum Hypotonic (< 275 mOsm/L)

Serum Sodium Falling (100 mOsm/L)

Urinary Sodium >30 mEq/L

Treatment

Fluid restriction

If Na < 120 mEq/L consider hypertonic saline to correct sodium (but no faster than 1

mEq/L/h) Intravenous urea Demeclocycline Lithium (rarely used)

Table from: http://openanesthesia.org/index.php?title=SIADH:_lab_findings

Serotonin syndrome (hi risks: SSRI +MAOI, SSRI + lithium, SSRI + TCA)

>> diarrhea, tremor, sweating, restlessness, hyperreflexia

progression of symptoms if untreated disorientation, rigidity, fever >> coma, seizures >> >> death (approximately 10%

mortality rate)

.Many medications/substances have serotonin activity:

dextromethorphan, fentanyl, meperidine, sumatriptan,

St Johns Wort, MDMA (ecstasy), LSD, many others

Consider total serotonergic load- Supplements (tryptophan, 5-HT), Herbs (St. Johns Wort),other antidepressants (venlafaxine, bupropion,

trazodone), other drugs with serotonergic effects (meperidine, dextromethorphan,and the triptans )

-------- In reality, usually only a problem with the pharmaceuticals.

NOTE on Drug-Drug Interaction and antidepressants
http://www.ncbi.nlm.nih.gov/pubmedhealth/PMH0000583/http://www.ncbi.nlm.nih.gov/pubmedhealth/PMH0000695/http://www.ncbi.nlm.nih.gov/pubmedhealth/PMH0000695/http://www.ncbi.nlm.nih.gov/pubmedhealth/PMH0000583/


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SSRI levels tend not to be altered by other drugs but can potentially increase levels (inhibit metabolism) of certain drugs . The drugs

that are most likely to do this include: fluoxetine, fluvoxamine, paroxetine. Specific drug-drug interactions are less important than

knowing SSRIS may inhibit P450 pathways of drugs sensitive to/dependent on P450 metabolism

Paroxetine- especially strong level of evidence for PTSD, short half life can set stage for withdrawal

Sertraline

Fluoxetine- Numerous drug-drug interactions, very long half life prevents withdrawal

Citalopram

Escitalopram- understand this is the S-isomer, the more biologically active molecule

Fluvoxamine

Nefazodone- irreversible liver toxicity

SNRIS (mild elevations in blood pressure, hyperhidrosis, tachycardia, decreased appetite, headache, insomnia, delayed ejaculation)

Atomoxetine- used primarily for attention/ADHD

Duloxetine- extensive data in pain, FDA approved for fibromyalgia

Venlafaxine- most effective antidepressant; severe withdrawal syndrome (anxiety, nausea, restlessness, irritability, electric shock paresthesias,

fatigue, headache, dizziness)

Dexvenlafaxine- metabolite of venlafaxine, idea was to create better steady state concentrations at lower doses therefore more potency with

fewer side effects- hasnt really held up to scrutiny


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Tricyclics (SNDRI)

Pharmacologically promiscuous:

Muscarinic M1 receptor antagonism - anticholinergic effects including altered mental status/confusion, resting tachycardia, dry mucous

membraines, dilated pupils, dizziness, emesis, constipation, urinary retention, flushed/hot skin, emesis, fever

Histamine H1 receptor antagonism - sedation and weight gain

Adrenergic receptor antagonism(NE) - postural hypotension

Direct membrane effects - reduced seizure threshold, arrhythmia

Serotonin 5-HT2 receptor antagonism - weight gain (and reduced anxiety)

NE 5HT Ach Sed (hist) Comments

amitriptyline (Elavil) low high high high pain, migraine, anxiety

clomipramine (Anafranil) low high high high tx OCD; SSRI-like FDA approval OCD

desipramine (Norpramin) high low low low activating

doxepin (Sinequan). low low mod high used for insomnia; very antihistaminic- used for hives, FDA approval insomnia

imipramine (Tofranil). low low mod mod pain; enuresis FDA approval enuresis

nortriptyline (Pamelor).. mod low mod mod chronic pain

protriptyline (Vivactil) high low mod low least sedating

MAOI Inhibitors


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Inhibit degradation of monaomines (norepinephrine, serotonin, melatonin, dopamine).

Phenelzine, Isocarboxazid, Tranylcypromine: non selective (MAO-A and B) and irreversible (enzyme is permanently inhibited and its activity will

not be replaced until body makes more). These non-selective irreversible drugs create dangerous situations if dietary intake of certain amines is

high. Tyramine= hypertensive crisis; foods rich in tyramine include Foods containing considerable amounts of tyramine include meats that areaged, smoked, pickled, mostpork (exceptcuredham),chocolate;alcoholic beverages;and fermented foods, such as

mostcheeses (exceptricotta,cottage,cream),sour cream,yogurt,shrimp paste,soy sauce,soybean condiments, tofu,tempeh,miso

soup,sauerkraut,broad (fava) beans,green bean pods,snowpeas,avocados,bananas,pineapple,eggplants,figs,peanuts,Brazil nuts,yeast.

Levodopa= psychosis, agitation, nausea; from fava beans

Selegiline- selective for MAOI-B; no dietary concerns at lower doses; become less selective at higher doses

Unique mechanism:

L-methylfolate; probably completely safe; especially useful in folks with MTHFR insufficiencies secondary to mutation

L-methylfolate is the precursor to serotonin, norepinephrine, dopamine, that is able to cross BBB. MTHFR in the brain then begins process that

ultimately leads to production of these psychoactive amines.

Seehttp://www.primarypsychiatry.com/aspx/articledetail.aspx?articleid=1938for nice article

Unique mechanism:

Bupropion

MOA: inhibition of presynaptic dopamine and norepinephrine reuptake transporters; Increased activity of vesicular monoamine transporter-2,

the transporter pumping dopamine and norepinephrine from the cytosol into presynaptic vesiclesFDA approved: smoking cessation (Zyban), Major Depression, Seasonal Affective Disorder

High Yield Facts:

Less sexual side effects (may actually help)

Less weight gain, may help with weight loss

Less likely to trigger mania than SSRIs

Doses over 300 mg associated with seizures

Unique mechanism:
http://en.wikipedia.org/wiki/Porkhttp://en.wikipedia.org/wiki/Curing_(food_preservation)http://en.wikipedia.org/wiki/Hamhttp://en.wikipedia.org/wiki/Chocolatehttp://en.wikipedia.org/wiki/Alcoholic_beveragehttp://en.wikipedia.org/wiki/Cheesehttp://en.wikipedia.org/wiki/Ricottahttp://en.wikipedia.org/wiki/Cottage_cheesehttp://en.wikipedia.org/wiki/Cream_cheesehttp://en.wikipedia.org/wiki/Sour_creamhttp://en.wikipedia.org/wiki/Yogurthttp://en.wikipedia.org/wiki/Shrimp_pastehttp://en.wikipedia.org/wiki/Soy_saucehttp://en.wikipedia.org/wiki/Soybeanhttp://en.wikipedia.org/wiki/Tofuhttp://en.wikipedia.org/wiki/Tempehhttp://en.wikipedia.org/wiki/Miso_souphttp://en.wikipedia.org/wiki/Miso_souphttp://en.wikipedia.org/wiki/Sauerkrauthttp://en.wikipedia.org/wiki/Vicia_fabahttp://en.wikipedia.org/wiki/Green_beanhttp://en.wikipedia.org/wiki/Snow_peahttp://en.wikipedia.org/wiki/Avocadohttp://en.wikipedia.org/wiki/Bananahttp://en.wikipedia.org/wiki/Pineapplehttp://en.wikipedia.org/wiki/Eggplanthttp://en.wikipedia.org/wiki/Ficushttp://en.wikipedia.org/wiki/Peanuthttp://en.wikipedia.org/wiki/Brazil_nuthttp://en.wikipedia.org/wiki/Yeasthttp://www.primarypsychiatry.com/aspx/articledetail.aspx?articleid=1938http://www.primarypsychiatry.com/aspx/articledetail.aspx?articleid=1938http://www.primarypsychiatry.com/aspx/articledetail.aspx?articleid=1938http://www.primarypsychiatry.com/aspx/articledetail.aspx?articleid=1938http://en.wikipedia.org/wiki/Yeasthttp://en.wikipedia.org/wiki/Brazil_nuthttp://en.wikipedia.org/wiki/Peanuthttp://en.wikipedia.org/wiki/Ficushttp://en.wikipedia.org/wiki/Eggplanthttp://en.wikipedia.org/wiki/Pineapplehttp://en.wikipedia.org/wiki/Bananahttp://en.wikipedia.org/wiki/Avocadohttp://en.wikipedia.org/wiki/Snow_peahttp://en.wikipedia.org/wiki/Green_beanhttp://en.wikipedia.org/wiki/Vicia_fabahttp://en.wikipedia.org/wiki/Sauerkrauthttp://en.wikipedia.org/wiki/Miso_souphttp://en.wikipedia.org/wiki/Miso_souphttp://en.wikipedia.org/wiki/Tempehhttp://en.wikipedia.org/wiki/Tofuhttp://en.wikipedia.org/wiki/Soybeanhttp://en.wikipedia.org/wiki/Soy_saucehttp://en.wikipedia.org/wiki/Shrimp_pastehttp://en.wikipedia.org/wiki/Yogurthttp://en.wikipedia.org/wiki/Sour_creamhttp://en.wikipedia.org/wiki/Cream_cheesehttp://en.wikipedia.org/wiki/Cottage_cheesehttp://en.wikipedia.org/wiki/Ricottahttp://en.wikipedia.org/wiki/Cheesehttp://en.wikipedia.org/wiki/Alcoholic_beveragehttp://en.wikipedia.org/wiki/Chocolatehttp://en.wikipedia.org/wiki/Hamhttp://en.wikipedia.org/wiki/Curing_(food_preservation)http://en.wikipedia.org/wiki/Pork


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Trazodone (priapism, low blood pressure)

binds at 5-HT2 receptor---

--acts as a serotonin agonist at high doses and a serotonin antagonist at low doses

--inhibits serotonin reuptake, as SSRIs

--It weakly blocks presynaptic alpha2-adrenergic receptors and strongly inhibits postsynaptic alpha1 receptors

DOES NOT affect the reuptake of norepinephrine or dopamine within the CNS.

Unique mechanism:

Mirtazepine (somnolence, increased appetite)

MOA: 1. antagonist at central pre-synaptic alpha(2)-receptors, inhibiting negative feedback to the presynaptic nerve and causing an increase in

NE release. 2. Agonist/antagonist at multiple sites:

------Blocks alpha(2)-receptors contained in serotenergic neurons, enhances the release of 5-HT which increased activity at at 5-HT and 5-HT1

which decreases anxiety

-----weak antagonist at 5-HT1receptors and as a potent antagonist at 5-HT2(particularly subtypes 2A and 2C) and 5-HT3receptors.

What you need to know: increases activity at some 5-HT, decreases at others, resulting in decreased anxiety---very effective anxiolytic

Drugs Used to Treat Psychosis and Agitation

Mechanism: All block dopamine with various affinities

Typical Antipsychotics:1.Phenothiazines:

a. Aliphatic side chain: Chlorpromazine

b. Piperidine side chain: Thioridazine

c. Piperazine side chain: Trifluoperazine, Fluphenazine

2.Butyrophenones: Haloperidol

3.Thioxanthenes: Thiothixene


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4. Other heterocyclics: Pimozide, Loxapine

High potency: fluphenazine, trifluoperizine, thiothixene, haloperidol, pimozide

medium-low sedation, high EPS, low AC

FTTHP: five truly terrible harsh pills

Low potency: chlorpromazine, mesoridazine, thioridazine

medium-high sedation, low-medium EPS, high AC

MCT: medications creating tiredness

Medium potency:perphenazine, loxapine, molindone

low-medium sedation, high EPS, low-medium AC

MLP: moderately lethal pills

EPS: extrapyramidal symptomsAC: anticholinergic effects

ALL OF THESE ARE EXTRAPYRAMIDAL SYMPTOMS

Acute dystonia

sustained muscular contraction of neck, eyes, throat

generally occurs soon after starting medication

Akathisia

uncomfortable continuous motor restlessness can occur any time in treatment but generally in first week(s)

easily misdiagnosed as the underlying psychiatric disorder

Treat with Beta Blocker primarily propranolol (must be lipid soluble)

Parkinsonism

tremor, muscle stiffness, slowed movement, drooling, masked face

generally occurs beyond 1 week after starting medication


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Tardive dyskinesia (TD)

spastic facial distortions and tongue movements, rhythmic small movements

may extend to neck, trunk, and extremities

delayed effect, usually beyond 6 months from starting medication

risk increases with duration of exposure to antipsychotic, lithium, age, other neurological diagnosis

known to occur without antipsychotic therapy

may be permanent, occur on discontinuation or resolve on own

Neuroleptic malignant syndrome (NMS)

pipe-like rigidity, fever, tremor, altered level of consciousness

hypotension, tachycardia

laboratory abnormalities- elevated WBC & CK

mortality 10-20%

can occur any time in course of treatment

SPECTRUM

Also, Anticholinergic effects (NOT EPS)

dry mouth, blurred vision, constipation, urinary retention, mydriasis (dilated pupils)

AND

Hyperlipidemia, weight gain, impaired glucose tolerance/diabetes

Haloperidol- treatment of choice for delirium, agitation

Chlorpromazineheavily sedating; approved for use in children

ThioridazineBlack Box QTc prolongation

Loxapine

Molindone

PerphenazineCATIE trial supported equivalent to atypicals
http://en.wikipedia.org/wiki/Chlorpromazinehttp://en.wikipedia.org/wiki/Thioridazinehttp://en.wikipedia.org/wiki/Loxapinehttp://en.wikipedia.org/wiki/Molindonehttp://en.wikipedia.org/wiki/Perphenazinehttp://en.wikipedia.org/wiki/Perphenazinehttp://en.wikipedia.org/wiki/Molindonehttp://en.wikipedia.org/wiki/Loxapinehttp://en.wikipedia.org/wiki/Thioridazinehttp://en.wikipedia.org/wiki/Chlorpromazine


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Thiothixene

Trifluoperazine

Fluphenazine

Prochlorperazine

Pimozide- approved for Tourettes

Atypical neuroleptics/antipsychotics: Dopamine blockade AND Serotonin blockade. Serotonin is like a brake to dopamine.

When you block dopamine, there are side effects from that blockade. BUT, when you also block receptor activity that is itself

braking dopamine, you ameliorate those effects.

Also used for:

schizophrenia and other psychotic disorders

acute bipolar mania & maintenance

augmentation of antidepressants & mood stabilizers

aggression & impulsivity

Risperidone- approved for aggression in autism, like typicals at high doses

Olanzapine- high likely diabetes/elevated lipids

Clozapine- agranulocytosis, seizure risks, diabetes/elevated lipids

Quetiapine- very low EPS risk

Asenapine

Ziprasidone- QTC prolongation
http://en.wikipedia.org/wiki/Thiothixenehttp://en.wikipedia.org/wiki/Trifluoperazinehttp://en.wikipedia.org/wiki/Fluphenazinehttp://en.wikipedia.org/wiki/Prochlorperazinehttp://en.wikipedia.org/wiki/Prochlorperazinehttp://en.wikipedia.org/wiki/Fluphenazinehttp://en.wikipedia.org/wiki/Trifluoperazinehttp://en.wikipedia.org/wiki/Thiothixene


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Iloperidone

Lurasidone- may have less propensity for negative effects on cognition

Aripiprazole- nausea, akithisia common side effects; other EPS very rare; DIFFERENT mechanism, sort of- works as partial agonist/antagonist,

potentially titrating its own dopamine blockade

Drugs Used to treat extrapyramidal symptoms

Anticholinergics All these treat extrapyramidal symptoms (EPS):

tremor, stiffness, drooling, dystonias

akathisia may not respond to ACs

tardive dyskinesia usually little response to ACs

Side effects all anticholinergic: fever, hot/flushed skin, constipation, blurred vision, urinary retention, dry mucous membranes

benztropine (Cogentin) M1 muscarinic acetylcholine receptor antagonist

least sedating, most commonly used

trihexyphenidyl (Artane): M1 muscarinic acetylcholine receptor antagonist

diphenhydramine (Benadryl) (antihistamine)


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Drugs Used to Improve Attention

Stimulants-

Side effects for stimulants are all the same = agitation/aggression, tics, tremors, seizures, increased adrenergic tone: tachycardia/blood pressure,sweating, mood swings, hyperthermia, psychosis

Amphetamines- block reuptake of norepinephrine and dopamine- when binding to presynaptic receptors, actually turn reuptake channels into

releasing channels

Dextroamphetamine

Levoamphetamine/Dextroamphetamine- mixed salts; contains both isomers

Lisdexamphetamine- prodrug; turns into dextroamphetamine upon cleavage of lysine; very long acting/smoother pharmacokinetic/dynamiccurves = less abuse potential

Methylphenidate- blocks reuptake of norepinephrine and dopamine

Dexmethylphenidate-dextrorotatory enantiomer ofmethylphenidate

Drugs Used to Promote Wakefulness

Unique mechanism of action: Modafinil
http://en.wikipedia.org/wiki/Dextrorotatoryhttp://en.wikipedia.org/wiki/Methylphenidatehttp://en.wikipedia.org/wiki/Methylphenidatehttp://en.wikipedia.org/wiki/Dextrorotatory


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Valproic Acid--- blocks high-frequency, repetitive neuronal firing by blocking voltage-dependent sodium channels, augment the action

of GAD (glutamic acid decarboxylase), a GABA-synthesizing enzyme, restricts GABA-T (GABA transaminase), an enzyme that speeds the

degradation of GABA.

can be dosed rapidly to treat acute mania

more effective than lithium in rapid cycling & mixed states

approved for migraine prophylaxis

serum levels can be helpful in guiding dosing, 70-100

nausea, weight gain, unsteadiness (ataxia), hair loss, tremor

liver dysfunction, decreased platelets (thrombocytopenia)

pancreatitis (rare but potentially serious)

polycystic ovary disease per reports

ammonia levels can be increased particularly in those rare individuals with genetic metabolic deficits

Carbamazepine.stabilizes the inactivated state ofVoltage-gated sodium channels,making fewer of these channels available to subsequently

openthe affected cells are less excitable untilthe drug dissociates.

GI: nausea, constipation, diarrhea, appetite loss

CNS: sedation, dizziness, unsteadiness, confusion

benign rashes common, catastrophic rashes rareStevens Johnson Syndrome- severe exfoliative erythematous rash with

systemic inflammation

many possible serious abnormalities in CBC- DECREASES..agranulocytosis
http://en.wikipedia.org/wiki/Voltage-gated_sodium_channelhttp://en.wikipedia.org/wiki/Voltage-gated_sodium_channelhttp://en.wikipedia.org/wiki/Voltage-gated_sodium_channel


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may reduce sodium levels (hyponatremia)

liver function abnormalities rare but possible

used in acute mania and bipolar maintenance..effectiveness within two weeks

more effective than lithium in rapid cycling & mixed states, less effective in bipolar related depression

serum levels to guide dosing, 4-12 mcg/ml

multiple significant drug-drug interactions (DDI) affecting both other medications (reducing their levels) & other medications

affecting it (increasing carbamazepine levels)

induces its own metabolism so may need to adjust dose over several weeks, half life decreases to 12-17 hours

DECREASES levels of OCPs, tricyclics, prednisone, Coumadin; fluoxetine, diltiazem, verapamil, erythromycin all INCREASE levels

of carbamazepine\

Oxcarbazepine

Does not have the enzyme-inducing effects of carbamazepine

tolerated better

Less drug-drug interactions

Hyponatremia, dizziness, ataxias, less blood dyscrasias

Lithium

Lithium has been found to decrease the activity and function of the Na+/K+/-ATPase pump in the CNS and especially in the

hippocampus.


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Lithium induced ADP ribosylation of the Gi G protein (therefore inactive).. increases basal levels of CAMP.at the same time, lithium

attenuates receptor-mediated activation of Adenylate Cyclase (AC) through a reduction in Gs subunit coupling. This results in a decrease

in the peak levels of stimulus induced CAMP. ?BALANCING EFFECT

rats....reduced levels of arachidonic acid and its products, which can contribute to inflammation AND increased levels of a metabolite

called 17-OH-DHA in response to inflammation. 17-OH-DHA is formed from the omega-3 fatty acid DHA (docosahexaenoic acid) and is

the precursor to a wide range of anti-inflammatory compounds known as docosanoids.

Lithium- features

Only mood stabilizer without significant anticonvulsant properties

up to 70% response rate

demonstrated effectiveness in reducing suicidality

less effective in rapid cycling and mixed bipolar states

serum levels guide dosing; above 1.3 toxic .7-1.2 therapeutic; above 3.5 dialyze

lab draw 8-12 hrs after last dose

excreted through the kidneys

minimal liver mediated drug-drug interactions (but see next slide for other medication issues)

Lithium- side effects

fine tremor, weight gain, nausea

increased thirst and urination

more severe toxicities include coarse tremor, gait instability, vomiting, diarrhea, confusion


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increased risk of toxicity with fluid or salt restriction, hot weather/sweating, use of anti-inflammatory drugs, ace inhibitors &

angiotensin receptor blockers, diuretics

may cause kidney and thyroid dysfunction so regular monitoring of creatinine, BUN and TSH are necessary

females /kids are at much greater risk of lithium related thyroid dysfunction

Lamotrigine----Inhibits voltage-dependent sodium channels, resulting in decreased release of theexcitatoryneurotransmitters glutamate and

aspartate.these act on NMDA receptors

Minimally sedating unlike most other mood stabilizers

Appears to be especially effective in bipolar depression.

Early use as an anticonvulsant in children raised concerns about potentially life-threatening rash (Stevens-Johnson syndrome

=toxic epidermal necrolysis).

Levetiracetam----binds to SV2A (synaptic vesicle protein 2A)..which is thought to.block conduction propagation (may also be from influences

on presynaptic calcium channels)

Topiramate--blockage of voltage-dependent sodium channels, augmentation of gamma-aminobutyrate acid activity at receptor, antagonism of

AMPA/kainate subtype at glutamate binding sites

Side effects: weight loss, cognitive dulling, kidney stones, metabolic acidosis, at moderate to high doses makes oral contraceptives ineffective

FDA Approved for MANIA

Aripiprazole

Carbamazepine

Chlorpromazine

Divalproex

Lithium

Olanzapine

Quetiapine

Risperidone

Ziprasidone

FDA Approved for Bipolar Maintenance
http://professionals.epilepsy.com/page/table_9steps_mechanism.htmlhttp://professionals.epilepsy.com/page/table_9steps_mechanism.htmlhttp://professionals.epilepsy.com/page/table_9steps_mechanism.htmlhttp://professionals.epilepsy.com/page/table_9steps_mechanism.html


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Lithium, Ziprasidone, Quetiapine, Risperidone, Aripiprazole, Olanzapine, Lamotrigine

Drugs Used to Treat DementiaUnique mechanism of action: Memantine (Namenda) ; moderate to severe

Blocks the toxic effects associated with excess glutamate and regulates glutamate activation- thought to block flow of current

through channels of N-methyl-d-aspartate (NMDA) receptors; may have more broad psychiatric application

Well done study supported some help in severe dementia

May be of more benefit in vascular dementia

Actylcholinesterase inhibitors

GI side effects are very common. Also insomnia. Rare but serious side effects include GI bleed. Benefits are modest. Thorough examination of

data suggests slowing of loss versus significant improvement.

donepezil (Aricept); approved for mild, moderate, and severe; minimal side effects

galantamine (Reminyl); mild to moderate; also stimulates nicotinic receptors

rivastigmine (Exelon); mild to moderate

tacrine (Cognex) not used due to liver toxicity


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Drugs Used to Treat Substance Abuse

buprenorphine/naloxone (Suboxone)

treatment for opioid dependence

diminishes cravings, evidence-based for maintenance of sobriety from opioids

contains both an agonist & antagonist----Buprenorphine: partial agonist activity at mu-opioid receptors, binds tightly and

prevents agonism of opioids Naloxone: antagonist; Naloxone was added to Suboxone in an effort to dissuade patients from

injecting the tablets---can trigger withdrawal, short half-life , attenuate any euphoria and abuse potential

naltrexone (ReVia)

opioid antagonist, longer half life and active metabolite makes it useful for treatment

Can trigger withdrawal if opioid dependent and using in last 7-10 days

Evidence for ETOH abstinence maintenancein combination with psychotherapy

Rationale for opioid abstinence but no data to support

potential liver toxicity

disulfiram (Antabuse) for ETOH abuse

deterrentmakes you sick


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