Term
|
Definition
| Antidepressant with tetracyclic structure. ADR include weight gain, constipation, xerostomia, dizziness, increased serum triglycerides. Has less sexual side effects compared to other antidepressants. |
|
|
Term
|
Definition
| Type of Monoamine Oxidase Inhibitor (MAOIs). Rarely used in clinical practice because of toxicity and potentially lethal food and drug interactions. Primarily used now for the treatment of depression unresponsive to other antidepressants. Can be used also to treat anxiety states, including social anxiety and panic disorder. |
|
|
Term
|
Definition
| A type of hydrazine derivative. Bind irreversibly and nonselectively with MAO-A and MAO-B. |
|
|
Term
| Adverse Effects of Phenelzine |
|
Definition
| Very slow elimination. Can cause hypotension, insomnia. Drug to drug interactions: can cause hypertensive crisis when combined with tyramine in the diet, or other indirect sympathomimetics. Can cause serotonin syndrome with serotonergic agents, along with some analgesic agents such as meperidine. |
|
|
Term
|
Definition
| CLASS: antipsychotic MOA: antagonizes dopamine D2 receptors in brain USES: Schizophrenia, N/V, Preoperative apprehension, Intraoperative sedation, intractable hiccups, acute intermittent porphyria, Migraine (off label). ADR: extrapyramidal sx, anticholinergic effects, sedation, weight gain, ED, oligomenorrhea or amenorrhea. Metabolism: Cleared by the liver MANY D/D interatctions! |
|
|
Term
|
Definition
| Benzodiazepine, anxiolytic, reduces neuronal depolarization resulting in decreased action potentials. Enhances the action of GABA by tightly binding to A-type GABA receptors, opening the membrane channels and allowing the entry of chloride ions. |
|
|
Term
|
Definition
| Antianxiety, muscle relaxants, procedural sedation agents, and sedative-hypnotics to treat withdrawal states (ex ETOH) and treat many hyperadrenergic/stimulated conditions (ex seizures, serotonin syndrome, neuroleptic malignant syndrome, sympathomimetic overdose, psychiatric conditions) |
|
|
Term
|
Definition
| CNS depression, take note of other medications that may increase this when administered together |
|
|
Term
|
Definition
| A heterocyclic or SNRI used in depression. Venlafaxine increases both serotonin and NE but mostly serotonin. May be more effective than other agents but must use larger doses. Do not use in combination with an SSRI or MAO inhibitors as this will substantially increase the patient's risk for serotonin syndrome. ADR include increased HR, BP, and CNS activation. Because of the increased CNS activation, patients may not sleep well if they take this medication too late in the day. Withdrawal syndrome is also a risk. May also see anticholinergic effects as well as sexual dysfunction. |
|
|
Term
|
Definition
| MOA not fully understood- inhibitors of norepinephrine and dopamine reuptake in animals. Increases presynaptic availability of catecholamine’s. No direct effect on serotonin. Unicyclic. |
|
|
Term
|
Definition
|
|
Term
|
Definition
| May be noradrenergic and/or dopaminergic |
|
|
Term
|
Definition
Huge first pass metabolism
Long halflife, once a day dosing.
. |
|
|
Term
|
Definition
Not thought to be effective for anxiety Major use for SAD, depression, used withother antidepressants to augment responses
Smoking cessation-
buproprion, seems to mimic nicotines effect on dopamine and norepinephrine
receptors.
.
least number of sexual side effects
no anti-cholinergic side effects and no weight gain |
|
|
Term
|
Definition
ADR: Nausea, agitation, insomnia, seizures with OD.
Contrindicated in pts with seizure hisotry. |
|
|
Term
|
Definition
| Prototype SSRI. MOA= block reuptake of serotonin, keeping higher serotonin levels at it's receptor site. Has a very long half life- does not need taper when d/c. Very minimal effect on other neurotransmitters |
|
|
Term
|
Definition
| Nausea and GI upset most common. Sexual dysfunction, decreased libido big disatisfier for pts. Can increase headaches and either insomnia or hypersomnia. Risk for serotonin syndrome, espeically in combo with other drugs that increase serotonin levels (ie: MAOIs). |
|
|
Term
|
Definition
anxiolytic psychoactive drug of the azapirone chemical class and is primarily
used to treat generalized anxiety disorder (GAD). |
|
|
Term
|
Definition
functions as a serotonin 5-HT1A receptor partial agonist. It
is this action that is thought to mediate its anxiolytic and antidepressant
effects. Additionally, it functions as a presynaptic dopamine agonist D2, D3,
dopamine antagonist D4, as well as a partial α1 receptor agonist. |
|
|
Term
|
Definition
| Most common adverse effects: drowsiness, upset stomach, vomiting, constipation, diarrhea, stomach pain, headache, dry mouth, depression, excitement, fatigue, nervousness, insomnia, lightheadedness, weakness, numbness. |
|
|
Term
Buspirone
contraindications |
|
Definition
Hypersensitivity to buspirone, metabolic
acidosis, as in diabetes, should not be used with MAO inhibitors, severely
compromised liver and/or renal function. Buspirone has been assigned to
pregnancy category B by the FDA. |
|
|
Term
|
Definition
| Binds selectively to GABA receptors to enhance membrane hyperpolarization. |
|
|
Term
| Zolpidem clinical effects and usage |
|
Definition
| Rapid onset of hypnosis with few amnesties effects or day after psychomotor depression or somnolence. Used in treatment of sleep disorders. |
|
|
Term
|
Definition
| blockade of D2 receptor, histamine and alpha |
|
|
Term
| Chlopromazine Clinical Uses |
|
Definition
| One of the oldest antipsycotics; used to treat schizophrenia, bipolar disorder, used more infrequently now d/t newer agents with less side effects |
|
|
Term
| Chlopromazine Pharmakinetics |
|
Definition
| given orally in 10-200mg tablets, can be given rectally and parenteral as well; systemic availability of 25-30%, undergoes significant first pass metabolism |
|
|
Term
| Chlopromazine Adverse Effects |
|
Definition
| very sedating, akathisia, dystonia, hyperprolactinemia, weight gain |
|
|
Term
|
Definition
| Used for Insomnia - It is a melatonin receptor agonist acting in vitro in cells expressing high selectivity for human MT1 & MT2 receptors compared to MT3 receptor, contributing to the sleep promoting properties. The receptors are thought to be part of the circadian rhythm maintenance underlying the sleep-wake cycle. |
|
|
Term
| Ramelteon - Rozerem - Pharm. |
|
Definition
| Absorption - 1/2 - 1 hour, Bioavailability - 1st Pass metabolism, Food delays absorption by 45 mins., High Fat meal increases AUC and Decreases Cmax, Distribution - Protein Binding, Metabolism - Liver, Excretion - Renal, 1/2 Life= 1 - 2.6 hours |
|
|
Term
| Ramelteon - Adverse Effects |
|
Definition
| Nausea, Dizziness, Fatigue, exacerbated Insomnia, Somnolence, worsen Depression, Hallucinations, Mania |
|
|
Term
|
Definition
| Binds to GABA receptor subunits in the central nervous system. This enhances membrane hyperpolarizaion and leads to a reduction in muscle spasticity. |
|
|
Term
|
Definition
| Treat chronic spasms from: cerebral palsy, stroke, spinal chord injury. Treatment of acute spams from a muscle injury. Treatment for anxiety, insomnia, or ETOH withdrawal. Given before procedures like cardiac catheterization or EGD to prevent spasms in coronary arteries or esophagus during the procedure. |
|
|
Term
|
Definition
| Sedation, dizziness, nausea, depression, reflex tachycardia, suppression of REM sleep |
|
|
Term
|
Definition
| Hepatic metabolism. Long half-life with a duration of 12-24 hours. However, short duration of action due to redistribution of lipophilic sites. |
|
|
Term
|
Definition
| A nonbenzodiazapine that is FDA approved for use as an anxiolytic. Also used off-label for Depression |
|
|
Term
|
Definition
| Exact MOA unclear. Chemically unrelated to other psychotropic medications. Buspirone appears to produce anxiolytic effects via serotonergic and dopaminergic effects. The drug lacks the anticonvulsant, sedative, and muscle relaxant effect of benzodiazepines, and has been termed "anxioselective". Buspirone does not bind to the benzodiazepine-GABA-chloride ion receptor complex in vitro. It has a significant effect on the dopaminergic system, interacting with dopamine receptors in vitro and acting pharmacologically as an agonist, antagonist, or both (in vivo and in vitro). |
|
|
Term
|
Definition
| Buspirone appears to block presynaptic dopamine receptors selectively and causes an increased firing rate in midbrain dopamine neurons. Lowers acetylcholine in selected parts of the brain, whereas benzodiazepines increase brain acetylcholine. It has been felt that the interaction of buspirone with dopaminergic pathways may account for its anxiolytic effects |
|
|
Term
|
Definition
| Appears generally well tolerated. Serious side-effects include CVA, CHF, and/or MI occurring in 0.1% of users. Dizziness appears to be most common occurring in 12% of users. |
|
|
Term
|
Definition
| Newer hypnotic that produces drowsiness, pronounced depression of CNS, and encourages the onset and maintenance of sleep |
|
|
Term
| Zolpidem pharmacokinetics |
|
Definition
| Oral; peak plasma concentration in 1.6hrs, half-life 1.5-3.5hrs. Rapidly metabolized. Excreted by kidney. Clearance is decreased in elderly |
|
|
Term
|
Definition
|
|
Term
|
Definition
| Selectively binds to molecular components of GABA alpha 1 subunit receptors in the neuronal membranes in the CNS |
|
|
Term
|
Definition
| Decreases REM sleep with little effect on slow-wave sleep. No anticonvulsant activity |
|
|
Term
| Zolpidem special considerations |
|
Definition
| Tolerance can occur with extended use. Withdrawl symptoms may occur with abrupt cessation |
|
|
Term
|
Definition
| MAOIs act by lessening the action of monoamine oxidase in the neuron and increases monoamine content. There are 2 forms of MAO: MAO-A (present in dopamine and norepinephrine found in the brain, gut, placenta, and liver; acts on norepinephrine, epinephrine, & serotonin) and MAO-B (found in serotonergic and histaminergic neurons located in the brain, liver, and platelets; acts on tyramine, phenylethylamine, & benzylamine).Blocks MAO-A and MAO-B irreversibly and non-selective |
|
|
Term
| Phenelzine Clinical Indications |
|
Definition
| Major depression unresponsive to other drugs |
|
|
Term
|
Definition
| Orthostatic Hypotension and weight gain, Anorgasmia, insomnia, restlessness, Confusion |
|
|
Term
|
Definition
Hypertensive crisis with tyramine and other indirect sympathomimetics
Serotonin syndrome with serotonergic agents |
|
|
Term
|
Definition
| provides moderately selective blockade of both norepinephrine transporter (NET) and serotonin transporter (SERT), resulting in an acute increase in serotonergic and adrenergic synaptic activity |
|
|
Term
| Venlafaxine Clinical Uses |
|
Definition
| *major depression*, chronic pain disorders, fibromyalgia, generalized anxiety, stress urinary incontinence, vasomotor symptoms of menopause |
|
|
Term
|
Definition
| anticholinergic effects, sedation, hypertension |
|
|
Term
|
Definition
| Increased norepinephrine and dopamine activity. Presynaptic release of catecholamines but no effect on 5-HT |
|
|
Term
|
Definition
| Major depression, smoking cessation |
|
|
Term
|
Definition
| lowers seizure threshold, suicidal thoughts/behavior, agitation, HA, dry mouth, N/V, tremor |
|
|
Term
|
Definition
| Antagonist of the presynaptic alpha 2 autoreceptors and enhances the release of both norepinephrine and 5-HT |
|
|
Term
| Mirtazapine Clinical Uses |
|
Definition
| Used for major depression; insomnia |
|
|
Term
|
Definition
| sedation(potent H1 antagonist wihc is associated with drugs sedative effects), weight gain, dizziness,not associated with sexual side effects like many of other drugs used for depression |
|
|
Term
|
Definition
|
|
Term
|
Definition
| selectively inhibits serotonin reuptake, therefore increasing the effects of serotonin at its receptor. Fluoxetine is metabolized to norfluoxetine its active product |
|
|
Term
|
Definition
| Depression, anxiety, OCD, bulimia nervosa, panic disorder |
|
|
Term
|
Definition
| GI, nausea, sexual dysfunction, seratonin syndrome |
|
|
Term
|
Definition
| Long 1/2 life (48-72 hours) Protein binding (95%), inhibits CYP3A4 |
|
|
Term
|
Definition
SNRI= serotonin-norepinephrine reuptake inhibitor
Stronger inhibitor of serotonin transporter (SERT) than norepinephrine transporter (NET). |
|
|
Term
|
Definition
Depression
Generalized Anxiety Disorder |
|
|
Term
|
Definition
Increased: heart rate, BP, CNS excitation
Withdrawal Syndrome
NEVER MIX VENLAFAXINE w/ SSRI- high risk for Serotonin Syndrome
(require high dose- >225mg/day... need to titrate) |
|
|
Term
|
Definition
SNRIs differ from TCAs in that SNRIs lack antihistamine, anti-adrenergic or anticholinergic effects of TCAs
(therefore SNRIs have less S/E and are better tolerated than TCAs) |
|
|
Term
|
Definition
(newer hyponotic) Selectively binds to BZ1 receptors, acting like benzodiazepines to enhance membrane hyperpolarization.
uses: sleep disorders |
|
|
Term
| Zolpidem (clinical considerations) |
|
Definition
Rapid onset, short duration
Miminal muscle relaxation and anticonvulsant effects
Lacks rebound insomnia |
|
|
Term
|
Definition
CNS depression
depression liability
Interactions with ethanol and other drugs - additive CNS depression |
|
|
Term
|
Definition
Is a serotoin agonist at the 5-HT receptor and likes to bind to the D2 receptor sites.
It's primary use is in generalized anxiety states (not good for painic attacks) and it does not cause sedation or hypnotic or euphoric effects.
May take over a week before effectiveness noted. |
|
|
Term
|
Definition
Common: Nausea, dizziness, headache, somnolence, nervousness sensation.
Serious (VERY RARE= less than 0.1%): CHF, CVA, & MI |
|
|
Term
|
Definition
| Benzodiazepine, skeletal mucscle relaxant, antianxiety, anticonvulsant, long half-life |
|
|
Term
|
Definition
| binds to GABA receptors to increase GABA's actions, tranquilization caused by inhibition of the limbic system |
|
|
Term
|
Definition
| Cardiac dysrthymias, confusion, respritory depression |
|
|
Term
|
Definition
| ETOH withdrawl, anxiety, seizures |
|
|
Term
|
Definition
| monoamine oxidase (MAO) inhibitor, hydrazine derivative binding irreversibly and nonselectively with MAO-A and -B |
|
|
Term
|
Definition
| Orthostatic Hypotension, abdominal discomfort, constipation, hypertensive crisis (as a result of tyramine build-up) |
|
|
Term
| phenelzine (Clinical Uses) |
|
Definition
| Depression; Non-FDA Labeled: Agoraphobia, Bulimia nervosa, Panic disorder, Social phobia |
|
|
Term
| Chlorpromazine (Thorazine) MOA |
|
Definition
| Dopamine 2 receptor > 5 HT2A receptor blockade |
|
|
Term
| Chlorpromazine (thorazine) clinical indices |
|
Definition
Oldest drug used for treatment of Schizophrenia
Also used for biopolar, antiemesis, preoperative sedation, pruritis |
|
|
Term
| Chlorpromazine (thorazine) ADR's |
|
Definition
Alpha, muscarinic and H1 receptor antagonistic effects as well
-CNS depression and major sedation, lowered seizure threshold, extrapyramidal effects (movement disorders), tardive dyskinesias, urinary retention, hyperprolactenemia, amenorrhea/infertility, weight gain |
|
|
Term
|
Definition
| A selective MT1 and MT2, metatonin agonist used to treat insomnia in patients having difficulty with sleep onset. Ramelteon's binding to the MT1 and MT2 receptors, which are normally acted upon by endogenous melatonin, contributes to sleep-promotion and maintenance of the circadian rhythm underlying the normal sleep-wake cycle. It has no effect on GABA. It is not addictive and it is not a controlled substance. FDA pregnancy category C. |
|
|
Term
| Ramelteon (Drug Interactions and Precautions) |
|
Definition
| It is metabolized by the P450 enzyme and should not be used when taking CYP1A2 inhibitors (ciprofloxacin, fluvoxamine, tacrine, zileuton) or CYP2C9 (Fluconaxole) and should be used in caution with patients with liver dysfunction. |
|
|
Term
|
Definition
| Dizziness, somnolence, fatigue, hallucinations, angioedema (rare). It may decrease testosterone and increase prolactin. A worsening of insomnia and depression may occur. |
|
|
Term
| Mirtazapine dosing considerations |
|
Definition
| Administer dose in the evening due to sedating effect (T1/2 is 20-40 hours) |
|
|
Term
|
Definition
| Weight gain very common, more of a sedative effect than other agents |
|
|
Term
|
Definition
| Combination 5HT2 and alpha adrenoceptor antagonist. Also is a potent H1 antagonist which is where the sedating effects are associated from |
|
|
Term
| Mirtazapine Clinical Uses |
|
Definition
| Major depressive disorder, as an adjunct to increase appetite in patients with AIDS or cancer |
|
|
Term
|
Definition
| Atypical antidepressant/smoking cessation aid, MOA poorly understood, weakly inhibits reuptake of DA and NE; suicide warning under age 24; does not cause sexual dysfunction; ↓seizure threshold, weight loss common |
|
|
Term
|
Definition
|
|
Term
|
Definition
| MOA poorly understood: may increase presynaptic availablity of catecholamines by inhibiting their reuptake (NE > Dopamine), may be a 5-HT1 agonist |
|
|
Term
|
Definition
| Major depression, adjunct in smoking cessation |
|
|
Term
|
Definition
| Nausea, headache, agitation, insomnia, anorexia, tachycardia |
|
|
Term
| History of seizures (lowers seizure threshold) |
|
Definition
| What is a contraindication to bupropion? |
|
|
Term
|
Definition
| Bupriopion is not FDA approved for which population? |
|
|
Term
|
Definition
| Bupriopion is which pregnancy category? |
|
|
Term
|
Definition
| Antidepresssant, Nonselective Monoamine Oxidase Inhibitor |
|
|
Term
|
Definition
| The exact mechanism of action has not been determined, it appears that the irreversible, nonselective inhibition of MAO by phenelzine relieves depressive symptoms by causing an increase in the levels of serotonin, norepinephrine, and dopamine in the neuron. |
|
|
Term
|
Definition
| Seizures, suicidal thoughts, hypertensive crisis, worsening depression, hepatic necrosis |
|
|
Term
|
Definition
| orthostatic hypotension, weight gain, constipation, Increased liver aminotransferase level, dizziness, headache, fatigue |
|
|
Term
|
Definition
| reduced depression and associated symptoms, blood pressure, worsening of depression, suicidality, or unusual changes in behavior. |
|
|
Term
| Phenelzine Contraindications |
|
Definition
| 1. concomitant use, or use within 10 days, of dibenzazepine derivatives (carbamazepine, cyclobenzaprine, tricyclic or tetracyclic antidepressants) . 2. diabetes - may increase insulin sensitivity. 3. hypertensive crises, which can be fatal or result in intracranial bleed - may present as palpitations or frequent headaches during therapy. 4. Schizophrenia - may cuase hyperstimulation and/or agitation. |
|
|
Term
| Phenelzine Foods to Avoid |
|
Definition
| chocolate, certain aged cheeses, Chianti and other aged red wines, vermouth, avocado, pickled fish, broad beans, beers, liver, smoked or pickled meats, snails, and yeast extracts. |
|
|
Term
| Phenelzine and Serotonin Syndrome |
|
Definition
| Serotonin syndrome may develop in patients taking MAOIs and illicit drugs, dextromethorphan, SSRIs, meperidine, and herbal supplements such as St John's Wort. |
|
|
Term
|
Definition
| Tetracyclic antidepressant (chemical structure and belongs to the piperazino-azepine group of compounds). |
|
|
Term
| Mirtazapine (Remeron) MOA |
|
Definition
| Increased release of norepinephrine, 5-HT |
|
|
Term
| Mirtazapine clinical indications |
|
Definition
| Major depressive disorder |
|
|
Term
|
Definition
| Agranulocytosis, cirrhosis of liver, depression exacerbation, grand mal seizure, neuroleptic malignant syndrome, neutropenia, serotonin syndrome, status epilepticus, suicidal thoughts, suicide |
|
|
Term
|
Definition
| One of the few antidepressants not commonly associated with sexual side effects. |
|
|
Term
|
Definition
| Extensive metabolism in liver. |
|
|
Term
|
Definition
|
|
Term
| Mirtazapine pregnancy category |
|
Definition
|
|
Term
|
Definition
| Many - need to monitor drug interactions and need to discontinue and flush these medications out of their system before therapy can begin. |
|
|
Term
|
Definition
| prototype for selective serotonin re-uptake inhibitors (SSRIs); most commonly prescribed antidepressants in clinical use |
|
|
Term
|
Definition
| blocks reuptake of serotonin by selectively inhibiting SERT, the serotonin transporter, thus enhancing the effects of serotonin at its receptor |
|
|
Term
|
Definition
| most common: nausea & sexual dysfunction; most serious: serotonin syndrome |
|
|
Term
|
Definition
| characterized by: HTN, hyperreflexia, tremor, clonus, hyperthermia, diarrhea, mydriasis, agitation, coma w/ onset within hours; predictable when SSRI in combo w/ other 5HT drugs, as well as antidepressants (i.e.: linezolid, ondansetron, St. John's Wort, tramadol) |
|
|
Term
|
Definition
| d/c offending drug; sedate; & possibly a 5HT antagonist like cyproheptadine |
|
|
Term
|
Definition
| characterized by: mostly GI symptoms, but also anxiety & irritability; occurs with many SSRI's but less so with fluoxetine because of its long T 1/2 |
|
|
Term
|
Definition
| extremely safe as a single agent when considering suicide risk |
|
|
Term
|
Definition
| preferred for maintenance therapy because of fewest serious side effects |
|
|
Term
| fluoxetine clinical effects |
|
Definition
| quickly increases serotonergic synaptic activity & more slowly changes signaling pathways & neurotropic activity |
|
|
Term
|
Definition
| easy use; safe in OD; tolerable; cost/generic; broad use |
|
|
Term
|
Definition
| TCAs; MAOIs; theophyline; carbamazepine; cisapride; NSAIDs |
|
|
Term
|
Definition
| major depression; social anxiety; panic disorder; PTSD; OCD; bulimia; premenstrual dysphoric disorder |
|
|
Term
|
Definition
| Vd=12-97%; highly protein bound= 95% ; bioavailability= 70%; available as isomers & formulated in racemic forms; longest 1/2 life= 48-72 hrs; active metabolite (norfluoxetine) w/ T 1/2=180 hrs; highly lipophilic; P450 interactions |
|
|
Term
|
Definition
| long T 1/2, so d/c 4-5 weeks before administer any MAOI to decrease risk of serotonin syndrome |
|
|
Term
|
Definition
| Few sexual side effects, no anticholinergic side effects, no weight gain |
|
|
Term
|
Definition
|
|
Term
|
Definition
| Bind selectively to a subgroup of GABA(A) receptors, acting like benzodiazepines to enhance membrane hyperpolarization |
|
|
Term
| Zolpidem Clinical Applications |
|
Definition
| Sleep disorders, especially those categorized by difficulty falling asleep |
|
|
Term
|
Definition
| Rapid onset of hypnosis with few amnestic effects or day after psychomotor depression or somnolence |
|
|
Term
| Who should doses of Zolpidem be decreased in? |
|
Definition
| Patients with hepatic impairment and elderly |
|
|
Term
| What can develop with extended use of zolpidem? |
|
Definition
|
|
Term
| Zolpidem Drug Interactions |
|
Definition
| Any CNS depressants, alcoholic beverages, opoid analgesics, and phenothiazines-which can lead to additive effects. Less obvious are the antihistamines, some antihypertensions and TCA’s (antidepressant class), d/t enhanced CNS depression |
|
|
Term
| Venlafaxine (Effexor) Drug Class |
|
Definition
| Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs) |
|
|
Term
|
Definition
| Moderately selective blockade of NET and SERT to increase serotonergic and adrenergic activity |
|
|
Term
| Venlafaxine Clinical Uses |
|
Definition
| Depression. Also approved for treatment of neuropathy, fibromyalgia, generalized anxiety, stress urinary incontinence, and vasomotor symptoms of menopause |
|
|
Term
| Venlafaxine Adverse Reactions |
|
Definition
| Increased blood pressure and heart rate, GI symptoms, and CNS activation such as insomnia, anxiety, and agitation |
|
|
Term
| Venlafaxine Drug Interactions |
|
Definition
| Never mix with a SSRI drug as this can greatly increase risk of serotonin syndrome |
|
|
Term
|
Definition
| Phenothiazine derivative; exact MOA is unknown. Chlorpromazine has strong anti-adrenergic activity (D2-receptor blockade) and weak anti-cholinergic activity (muscarinic-receptor blockade). Also a weak blocker of serotonin (5HT2A) and H1 receptors. |
|
|
Term
| Chlorpromazine Toxicities |
|
Definition
| Toxic effects result from the anticholinergic properties of this drug (excessive sedation), as well as the alpha-blocking effects (hypotension) and mild sodium channel blocking effects (QRS prolongation and dysrhythmias). |
|
|
Term
| Chlorpromazine Pharmacokinetics |
|
Definition
| Up to 99% bound to protein, metabolized by liver, excreted by kidneys. Very long T1/2. |
|
|
Term
| Clinical Uses of Chlorpromazine |
|
Definition
| Antipsychotic agent used for schizophrenia and bipolar disorder (produces CNS depression). Also used as an antiemetic (due to dopamine-receptor blockade) and for itching (due to H1-receptor blockade). |
|
|
Term
|
Definition
| Extrapyramidal effects such as dystonia, tardive dyskinesia, akathisia, and Parkinson’s syndrome (tremor). Also dry mouth, urinary retention. |
|
|
Term
|
Definition
|
|
Term
|
Definition
| Anxiolytix, miscellaneous |
|
|
Term
|
Definition
| generalized anxiety disorder. Off label: augments anti depressants |
|
|
Term
|
Definition
| Unknown, Buspirone is a serotonin 5-HT1A and 5-HT2 agonist, without affecting GABA receptors |
|
|
