Term
|
Definition
Class: MAO-I (hydrazine derivative)
MOA: Irreversibly or reversibly inhibit both forms of MAO, causing accumulation of serotonin, NE, and dopamine
Clinical uses:
Last resort for depression (patients unresponsive to other antidepressants)
Depression with strong anxiety
Tx phobic states
Atypical depression (over-active rejection)
Low psychomotor activity
Bulimia and cocaine addiction (unlabeled)
Side effects:
Orthostatic hypotension
CNS stimulant effects (tremors, excitement, insomnia, increased appetite-->weight gain)
Atropine-like (anticholinergic) effects: dry mouth, constipation, etc.
Phenelzine only: severe hepatotoxicity
Interactions
"Cheese Reaction": Cheese, chicken liver, beer, red wine, and grapes produce tyramine, which is usually metabolized by MAO. On MAO-Is, tyramine enters the bloodstream, causing catecholamine release.
Symptoms: headache, tachycardia, nausea, HTN, cardiac arrhythmia, stroke
Treatment: Phentolamine, Prazosin
Reduce clearance of ephedrine and amphetamine
Symptoms: HTN, behavioral excitation
Synergistic effect with TCAs
Symptoms: Headache, SOB, heart attack or stroke, eclampsia (hypertensive crisis)
Interaction with pethidine/meperidine (opioid analgesic)
Symptoms: hyperpyrexia, restlessness, muscle rigidity, coma, vascular collapse
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Term
|
Definition
Class: MAO-I (non-hydrazine)
MOA: Irreversibly or reversibly inhibit both forms of MAO, causing accumulation of serotonin, NE, and dopamine
Clinical uses:
Last resort for depression (patients unresponsive to other antidepressants)
Depression with strong anxiety
Tx phobic states
Atypical depression (over-active rejection)
Low psychomotor activity
Bulimia and cocaine addiction (unlabeled)
Side effects:
Orthostatic hypotension
CNS stimulant effects (tremors, excitement, insomnia, increased appetite-->weight gain)
Atropine-like (anticholinergic) effects: dry mouth, constipation, etc.
Interactions
"Cheese Reaction": Cheese, chicken liver, beer, red wine, and grapes produce tyramine, which is usually metabolized by MAO. On MAO-Is, tyramine enters the bloodstream, causing catecholamine release.
Symptoms: headache, tachycardia, nausea, HTN, cardiac arrhythmia, stroke
Treatment: Phentolamine, Prazosin
Reduce clearance of ephedrine and amphetamine
Symptoms: HTN, behavioral excitation
Synergistic effect with TCAs
Symptoms: Headache, SOB, heart attack or stroke, eclampsia (hypertensive crisis)
Interaction with pethidine/meperidine (opioid analgesic)
Symptoms: hyperpyrexia, restlessness, muscle rigidity, coma, vascular collapse
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Term
|
Definition
Class: MAO-I (non-hydrazine)
MOA: Irreversibly or reversibly inhibit both forms of MAO (MAO-B only at low dose for selegiline only), causing accumulation of serotonin, NE, and dopamine
Clinical uses:
Last resort for depression (patients unresponsive to other antidepressants)
Depression with strong anxiety
Tx phobic states
Atypical depression (over-active rejection)
Low psychomotor activity
Bulimia and cocaine addiction (unlabeled)
Selegiline only: Parkinson's disesae treatment at low dose
Side effects:
Orthostatic hypotension
CNS stimulant effects (tremors, excitement, insomnia, increased appetite-->weight gain)
Atropine-like (anticholinergic) effects: dry mouth, constipation, etc.
Interactions
"Cheese Reaction": Cheese, chicken liver, beer, red wine, and grapes produce tyramine, which is usually metabolized by MAO. On MAO-Is, tyramine enters the bloodstream, causing catecholamine release.
Symptoms: headache, tachycardia, nausea, HTN, cardiac arrhythmia, stroke
Treatment: Phentolamine, Prazosin
Reduce clearance of ephedrine and amphetamine
Symptoms: HTN, behavioral excitation
Synergistic effect with TCAs
Symptoms: Headache, SOB, heart attack or stroke, eclampsia (hypertensive crisis)
Interaction with pethidine/meperidine (opioid analgesic)
Symptoms: hyperpyrexia, restlessness, muscle rigidity, coma, vascular collapse
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Term
|
Definition
Class: Tricyclic Antidepressant
MOA:
Competitively binds to amine transporter, preventing NE and serotonin reuptake
Binds muscarinic ACh receptor, α-adrenoceptor, histamine receptors, and serotonin receptor, leading to side effects
Clinical uses:
Major depression, especially with psychomotor features such as insomnia or poor appetite (amitriptyline)
Panic and related disorders
Neuropathic (chronic) pain (amitriptyline and imipramine)
Blocks NE and serotonin reuptake in ascending corticospinal monoamine pathway
Side effects:
Blockade of histamine receptor:
Excessive sedation (most common SE)
Lassitude
Fatigue
Confusion
Drowsiness
Loss of motor coordination
Blockade of M receptor (especially amitriptyline)
Blockade of α-adrenoceptor:
Postural hypotension (Strong effect)
Reflex cardiac tachycardia
Sympathomimetic effects (d/t increased catecholamine activity):
Tachycardia
Sweating
Agitation
Insomnia
Other:
Tremor
Paresthesia
Weight gain
Sexual dysfunction
Overdose: "3 C's": convulsions, coma, and cardiotoxicity
Interactions
Drugs that compete for hepatic metabolism (CYP2D6)
Antipsychotics: fluoxetine, paroxetine, bupropion, duloxetine, haloperidol, quinidine
Steroids
Synergistic Effect (Additive CNS depression):
Ethanol
Barbituates
Benzodiazepines
Opioids
Interfere with some antihypertensive medications because both have hypotensive effect
Guanethidine
Methylnorepinephrine
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|
|
Term
|
Definition
Class: Tricyclic Antidepressant
MOA:
Competitively binds to amine transporter, preventing NE and serotonin reuptake
Binds muscarinic ACh receptor, α-adrenoceptor, histamine receptors, and serotonin receptor, leading to side effects
Clinical uses:
Panic and related disorders (clomipramine for obsessional and phobic states)
Side effects:
Blockade of histamine receptor:
Excessive sedation (most common SE)
Lassitude
Fatigue
Confusion
Drowsiness
Loss of motor coordination
Blockade of M receptor (especially amitriptyline)
Blockade of α-adrenoceptor:
Postural hypotension (Strong effect)
Reflex cardiac tachycardia
Sympathomimetic effects (d/t increased catecholamine activity):
Tachycardia
Sweating
Agitation
Insomnia
Other:
Tremor
Paresthesia
Weight gain
Sexual dysfunction
Overdose: "3 C's": convulsions, coma, and cardiotoxicity
Interactions
Drugs that compete for hepatic metabolism (CYP2D6)
Antipsychotics: fluoxetine, paroxetine, bupropion, duloxetine, haloperidol, quinidine
Steroids
Synergistic Effect (Additive CNS depression):
Ethanol
Barbituates
Benzodiazepines
Opioids
Interfere with some antihypertensive medications because both have hypotensive effect
Guanethidine
Methylnorepinephrine |
|
|
Term
|
Definition
Class: Tricyclic Antidepressant
MOA:
Competitively binds to amine transporter, preventing NE and serotonin reuptake
Binds muscarinic ACh receptor, α-adrenoceptor, histamine receptors, and serotonin receptor, leading to side effects
Clinical uses:
Major depression, especially with psychomotor features such as insomnia or poor appetite (amitriptyline)
Panic and related disorders
Neuropathic (chronic) pain (amitriptyline and imipramine)
Blocks NE and serotonin reuptake in ascending corticospinal monoamine pathway
Nocturnal enuresis (imipramine and nortriptyline)
ADHD (imipramine, desipramine, nortriptyline)
Side effects:
Blockade of histamine receptor:
Excessive sedation (most common SE)
Lassitude
Fatigue
Confusion
Drowsiness
Loss of motor coordination
Blockade of M receptor (especially amitriptyline)
Blockade of α-adrenoceptor:
Postural hypotension (Strong effect)
Reflex cardiac tachycardia
Sympathomimetic effects (d/t increased catecholamine activity):
Tachycardia
Sweating
Agitation
Insomnia
Other:
Tremor
Paresthesia
Weight gain
Sexual dysfunction
Overdose: "3 C's": convulsions, coma, and cardiotoxicity
Interactions
Drugs that compete for hepatic metabolism (CYP2D6)
Antipsychotics: fluoxetine, paroxetine, bupropion, duloxetine, haloperidol, quinidine
Steroids
Synergistic Effect (Additive CNS depression):
Ethanol
Barbituates
Benzodiazepines
Opioids
Interfere with some antihypertensive medications because both have hypotensive effect
Guanethidine
Methylnorepinephrine |
|
|
Term
|
Definition
Class: Tricyclic Antidepressant
MOA:
Competitively binds to amine transporter, preventing NE and serotonin reuptake
Binds muscarinic ACh receptor, α-adrenoceptor, histamine receptors, and serotonin receptor, leading to side effects
Clinical uses:
Major depression, especially with psychomotor features such as insomnia or poor appetite (amitriptyline)
Panic and related disorders
Neuropathic (chronic) pain (amitriptyline and imipramine)
Blocks NE and serotonin reuptake in ascending corticospinal monoamine pathway
Nocturnal enuresis (imipramine and nortriptyline)
ADHD (imipramine, desipramine, nortriptyline)
Side effects:
Blockade of histamine receptor:
Excessive sedation (most common SE)
Lassitude
Fatigue
Confusion
Drowsiness
Loss of motor coordination
Blockade of M receptor (especially amitriptyline)
Blockade of α-adrenoceptor:
Postural hypotension (Strong effect)
Reflex cardiac tachycardia
Sympathomimetic effects (d/t increased catecholamine activity):
Tachycardia
Sweating
Agitation
Insomnia
Other:
Tremor
Paresthesia
Weight gain
Sexual dysfunction
Overdose: "3 C's": convulsions, coma, and cardiotoxicity
Interactions
Drugs that compete for hepatic metabolism (CYP2D6)
Antipsychotics: fluoxetine, paroxetine, bupropion, duloxetine, haloperidol, quinidine
Steroids
Synergistic Effect (Additive CNS depression):
Ethanol
Barbituates
Benzodiazepines
Opioids
Interfere with some antihypertensive medications because both have hypotensive effect
Guanethidine
Methylnorepinephrine |
|
|
Term
|
Definition
Class: Tricyclic Antidepressant
MOA:
Competitively binds to amine transporter, preventing NE and serotonin reuptake
Binds muscarinic ACh receptor, α-adrenoceptor, histamine receptors, and serotonin receptor, leading to side effects
Clinical uses:
Major depression, especially with psychomotor features such as insomnia or poor appetite (amitriptyline)
Panic and related disorders
Neuropathic (chronic) pain (amitriptyline and imipramine)
Blocks NE and serotonin reuptake in ascending corticospinal monoamine pathway
Nocturnal enuresis (imipramine and nortriptyline)
ADHD (imipramine, desipramine, nortriptyline)
Side effects:
Blockade of histamine receptor:
Excessive sedation (most common SE)
Lassitude
Fatigue
Confusion
Drowsiness
Loss of motor coordination
Blockade of M receptor (especially amitriptyline)
Blockade of α-adrenoceptor:
Postural hypotension (Strong effect)
Reflex cardiac tachycardia
Sympathomimetic effects (d/t increased catecholamine activity):
Tachycardia
Sweating
Agitation
Insomnia
Other:
Tremor
Paresthesia
Weight gain
Sexual dysfunction
Overdose: "3 C's": convulsions, coma, and cardiotoxicity
Interactions
Drugs that compete for hepatic metabolism (CYP2D6)
Antipsychotics: fluoxetine, paroxetine, bupropion, duloxetine, haloperidol, quinidine
Steroids
Synergistic Effect (Additive CNS depression):
Ethanol
Barbituates
Benzodiazepines
Opioids
Interfere with some antihypertensive medications because both have hypotensive effect
Guanethidine
Methylnorepinephrine |
|
|
Term
|
Definition
Class: Tricyclic Antidepressant
MOA:
Competitively binds to amine transporter, preventing NE and serotonin reuptake
Binds muscarinic ACh receptor, α-adrenoceptor, histamine receptors, and serotonin receptor, leading to side effects
Clinical uses:
Major depression, especially with psychomotor features such as insomnia or poor appetite (amitriptyline)
Panic and related disorders
Neuropathic (chronic) pain (amitriptyline and imipramine)
Blocks NE and serotonin reuptake in ascending corticospinal monoamine pathway
Nocturnal enuresis (imipramine and nortriptyline)
ADHD (imipramine, desipramine, nortriptyline)
Side effects:
Blockade of histamine receptor:
Excessive sedation (most common SE)
Lassitude
Fatigue
Confusion
Drowsiness
Loss of motor coordination
Blockade of M receptor (especially amitriptyline)
Blockade of α-adrenoceptor:
Postural hypotension (Strong effect)
Reflex cardiac tachycardia
Sympathomimetic effects (d/t increased catecholamine activity):
Tachycardia
Sweating
Agitation
Insomnia
Other:
Tremor
Paresthesia
Weight gain
Sexual dysfunction
Overdose: "3 C's": convulsions, coma, and cardiotoxicity
Interactions
Drugs that compete for hepatic metabolism (CYP2D6)
Antipsychotics: fluoxetine, paroxetine, bupropion, duloxetine, haloperidol, quinidine
Steroids
Synergistic Effect (Additive CNS depression):
Ethanol
Barbituates
Benzodiazepines
Opioids
Interfere with some antihypertensive medications because both have hypotensive effect
Guanethidine
Methylnorepinephrine |
|
|
Term
|
Definition
Class: Tricyclic Antidepressant
MOA:
Competitively binds to amine transporter, preventing NE and serotonin reuptake
Binds muscarinic ACh receptor, α-adrenoceptor, histamine receptors, and serotonin receptor, leading to side effects
Clinical uses:
Major depression, especially with psychomotor features such as insomnia or poor appetite (amitriptyline)
Panic and related disorders
Neuropathic (chronic) pain (amitriptyline and imipramine)
Blocks NE and serotonin reuptake in ascending corticospinal monoamine pathway
Nocturnal enuresis (imipramine and nortriptyline)
ADHD (imipramine, desipramine, nortriptyline)
Side effects:
Blockade of histamine receptor:
Excessive sedation (most common SE)
Lassitude
Fatigue
Confusion
Drowsiness
Loss of motor coordination
Blockade of M receptor (especially amitriptyline)
Blockade of α-adrenoceptor:
Postural hypotension (Strong effect)
Reflex cardiac tachycardia
Sympathomimetic effects (d/t increased catecholamine activity):
Tachycardia
Sweating
Agitation
Insomnia
Other:
Tremor
Paresthesia
Weight gain
Sexual dysfunction
Overdose: "3 C's": convulsions, coma, and cardiotoxicity
Interactions
Drugs that compete for hepatic metabolism (CYP2D6)
Antipsychotics: fluoxetine, paroxetine, bupropion, duloxetine, haloperidol, quinidine
Steroids
Synergistic Effect (Additive CNS depression):
Ethanol
Barbituates
Benzodiazepines
Opioids
Interfere with some antihypertensive medications because both have hypotensive effect
Guanethidine
Methylnorepinephrine |
|
|
Term
|
Definition
Class: Tricyclic Antidepressant
MOA:
Competitively binds to amine transporter, preventing NE and serotonin reuptake
Binds muscarinic ACh receptor, α-adrenoceptor, histamine receptors, and serotonin receptor, leading to side effects
Clinical uses:
Major depression, especially with psychomotor features such as insomnia or poor appetite (amitriptyline)
Panic and related disorders
Neuropathic (chronic) pain (amitriptyline and imipramine)
Blocks NE and serotonin reuptake in ascending corticospinal monoamine pathway
Nocturnal enuresis (imipramine and nortriptyline)
ADHD (imipramine, desipramine, nortriptyline)
Side effects:
Blockade of histamine receptor:
Excessive sedation (most common SE)
Lassitude
Fatigue
Confusion
Drowsiness
Loss of motor coordination
Blockade of M receptor (especially amitriptyline)
Blockade of α-adrenoceptor:
Postural hypotension (Strong effect)
Reflex cardiac tachycardia
Sympathomimetic effects (d/t increased catecholamine activity):
Tachycardia
Sweating
Agitation
Insomnia
Other:
Tremor
Paresthesia
Weight gain
Sexual dysfunction
Overdose: "3 C's": convulsions, coma, and cardiotoxicity
Interactions
Drugs that compete for hepatic metabolism (CYP2D6)
Antipsychotics: fluoxetine, paroxetine, bupropion, duloxetine, haloperidol, quinidine
Steroids
Synergistic Effect (Additive CNS depression):
Ethanol
Barbituates
Benzodiazepines
Opioids
Interfere with some antihypertensive medications because both have hypotensive effect
Guanethidine
Methylnorepinephrine |
|
|
Term
|
Definition
Class: Tricyclic Antidepressant
MOA:
Competitively binds to amine transporter, preventing NE and serotonin reuptake
Binds muscarinic ACh receptor, α-adrenoceptor, histamine receptors, and serotonin receptor, leading to side effects
Clinical uses:
Major depression, especially with psychomotor features such as insomnia or poor appetite (amitriptyline)
Panic and related disorders
Neuropathic (chronic) pain (amitriptyline and imipramine)
Blocks NE and serotonin reuptake in ascending corticospinal monoamine pathway
Nocturnal enuresis (imipramine and nortriptyline)
ADHD (imipramine, desipramine, nortriptyline)
Side effects:
Blockade of histamine receptor:
Excessive sedation (most common SE)
Lassitude
Fatigue
Confusion
Drowsiness
Loss of motor coordination
Blockade of M receptor (especially amitriptyline)
Blockade of α-adrenoceptor:
Postural hypotension (Strong effect)
Reflex cardiac tachycardia
Sympathomimetic effects (d/t increased catecholamine activity):
Tachycardia
Sweating
Agitation
Insomnia
Other:
Tremor
Paresthesia
Weight gain
Sexual dysfunction
Overdose: "3 C's": convulsions, coma, and cardiotoxicity
Interactions
Drugs that compete for hepatic metabolism (CYP2D6)
Antipsychotics: fluoxetine, paroxetine, bupropion, duloxetine, haloperidol, quinidine
Steroids
Synergistic Effect (Additive CNS depression):
Ethanol
Barbituates
Benzodiazepines
Opioids
Interfere with some antihypertensive medications because both have hypotensive effect
Guanethidine
Methylnorepinephrine |
|
|
Term
|
Definition
Class: Tricyclic Antidepressant
MOA:
Competitively binds to amine transporter, preventing NE and serotonin reuptake
Binds muscarinic ACh receptor, α-adrenoceptor, histamine receptors, and serotonin receptor, leading to side effects
Clinical uses:
Major depression, especially with psychomotor features such as insomnia or poor appetite (amitriptyline)
Panic and related disorders
Neuropathic (chronic) pain (amitriptyline and imipramine)
Blocks NE and serotonin reuptake in ascending corticospinal monoamine pathway
Nocturnal enuresis (imipramine and nortriptyline)
ADHD (imipramine, desipramine, nortriptyline)
Side effects:
Blockade of histamine receptor:
Excessive sedation (most common SE)
Lassitude
Fatigue
Confusion
Drowsiness
Loss of motor coordination
Blockade of M receptor (especially amitriptyline)
Blockade of α-adrenoceptor:
Postural hypotension (Strong effect)
Reflex cardiac tachycardia
Sympathomimetic effects (d/t increased catecholamine activity):
Tachycardia
Sweating
Agitation
Insomnia
Other:
Tremor
Paresthesia
Weight gain
Sexual dysfunction
Overdose: "3 C's": convulsions, coma, and cardiotoxicity
Interactions
Drugs that compete for hepatic metabolism (CYP2D6)
Antipsychotics: fluoxetine, paroxetine, bupropion, duloxetine, haloperidol, quinidine
Steroids
Synergistic Effect (Additive CNS depression):
Ethanol
Barbituates
Benzodiazepines
Opioids
Interfere with some antihypertensive medications because both have hypotensive effect
Guanethidine
Methylnorepinephrine |
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Term
|
Definition
Class: Selective Serotonin Reuptake Inhibitor (SSRI)
MOA:
Block 5-HT reuptake transporter in presynaptic terminals
Take two weeks for max benefit
Renal excretion except paroxetine and sertraline!
Fluoxetine has longest half life
Clinical uses:
Drug of choice for treatment of depression!
Generalized anxiety
Panic attacks
OCD (fluvoxamine)
Premenstrual dysphoric disorder- PMDD (fluoxetine and sertraline)
Bulimia (fluoxetine)
Side effects:
GI (n/v/d) most common
Sleep disturbances:
Paroxetine and fluvoxamine- sedating
Fluoxetine- activating
Sexual dysfunction
Withdrawal: nausea, dizziness, anxiety, tremor, palpitations
INX:
Fluoxetine and paroxetine inhibit CYP2D6 (reduce TCA elimination)
Citalopram causes fewer drug INX
Serotonin Syndrome when given with MAO-I
Tremor, myoclonus, muscle rigidity, hyperthermia, and cardio collapse
Tx: Antiseizure drug, muscle relaxant, 5-HT blocker (cyproheptadine)
Fluoxetine should be d/c'd for 4-5 weeks before MAO-I given
MAO-I d/c'd 2 weeks before SSRI
Overdose:
Seizures (fluoxetine) |
|
|
Term
|
Definition
Class: Selective Serotonin Reuptake Inhibitor (SSRI)
MOA:
Block 5-HT reuptake transporter in presynaptic terminals
Take two weeks for max benefit
Renal excretion except paroxetine and sertraline!
Fluoxetine has longest half life
Clinical uses:
Drug of choice for treatment of depression!
Generalized anxiety
Panic attacks
OCD (fluvoxamine)
Premenstrual dysphoric disorder- PMDD (fluoxetine and sertraline)
Bulimia (fluoxetine)
Side effects:
GI (n/v/d) most common
Sleep disturbances:
Paroxetine and fluvoxamine- sedating
Fluoxetine- activating
Sexual dysfunction
Withdrawal: nausea, dizziness, anxiety, tremor, palpitations
INX:
Fluoxetine and paroxetine inhibit CYP2D6 (reduce TCA elimination)
Citalopram causes fewer drug INX
Serotonin Syndrome when given with MAO-I
Tremor, myoclonus, muscle rigidity, hyperthermia, and cardio collapse
Tx: Antiseizure drug, muscle relaxant, 5-HT blocker (cyproheptadine)
Fluoxetine should be d/c'd for 4-5 weeks before MAO-I given
MAO-I d/c'd 2 weeks before SSRI
Overdose:
Seizures (fluoxetine)
|
|
|
Term
|
Definition
Class: Selective Serotonin Reuptake Inhibitor (SSRI)
MOA:
Block 5-HT reuptake transporter in presynaptic terminals
Take two weeks for max benefit
Renal excretion except paroxetine and sertraline!
Fluoxetine has longest half life
Clinical uses:
Drug of choice for treatment of depression!
Generalized anxiety
Panic attacks
OCD (fluvoxamine)
Premenstrual dysphoric disorder- PMDD (fluoxetine and sertraline)
Bulimia (fluoxetine)
Side effects:
GI (n/v/d) most common
Sleep disturbances:
Paroxetine and fluvoxamine- sedating
Fluoxetine- activating
Sexual dysfunction
Withdrawal: nausea, dizziness, anxiety, tremor, palpitations
INX:
Fluoxetine and paroxetine inhibit CYP2D6 (reduce TCA elimination)
Citalopram causes fewer drug INX
Serotonin Syndrome when given with MAO-I
Tremor, myoclonus, muscle rigidity, hyperthermia, and cardio collapse
Tx: Antiseizure drug, muscle relaxant, 5-HT blocker (cyproheptadine)
Fluoxetine should be d/c'd for 4-5 weeks before MAO-I given
MAO-I d/c'd 2 weeks before SSRI
Overdose:
Seizures (fluoxetine)
|
|
|
Term
|
Definition
Class: Selective Serotonin Reuptake Inhibitor (SSRI)
MOA:
Block 5-HT reuptake transporter in presynaptic terminals
Take two weeks for max benefit
Renal excretion except paroxetine and sertraline!
Fluoxetine has longest half life
Clinical uses:
Drug of choice for treatment of depression!
Generalized anxiety
Panic attacks
OCD (fluvoxamine)
Premenstrual dysphoric disorder- PMDD (fluoxetine and sertraline)
Bulimia (fluoxetine)
Side effects:
GI (n/v/d) most common
Sleep disturbances:
Paroxetine and fluvoxamine- sedating
Fluoxetine- activating
Sexual dysfunction
Withdrawal: nausea, dizziness, anxiety, tremor, palpitations
INX:
Fluoxetine and paroxetine inhibit CYP2D6 (reduce TCA elimination)
Citalopram causes fewer drug INX
Serotonin Syndrome when given with MAO-I
Tremor, myoclonus, muscle rigidity, hyperthermia, and cardio collapse
Tx: Antiseizure drug, muscle relaxant, 5-HT blocker (cyproheptadine)
Fluoxetine should be d/c'd for 4-5 weeks before MAO-I given
MAO-I d/c'd 2 weeks before SSRI
Overdose:
Seizures (fluoxetine)
|
|
|
Term
|
Definition
Class: Selective Serotonin Reuptake Inhibitor (SSRI)
MOA:
Block 5-HT reuptake transporter in presynaptic terminals
Take two weeks for max benefit
Renal excretion except paroxetine and sertraline!
Fluoxetine has longest half life
Clinical uses:
Drug of choice for treatment of depression!
Generalized anxiety
Panic attacks
OCD (fluvoxamine)
Premenstrual dysphoric disorder- PMDD (fluoxetine and sertraline)
Bulimia (fluoxetine)
Side effects:
GI (n/v/d) most common
Sleep disturbances:
Paroxetine and fluvoxamine- sedating
Fluoxetine- activating
Sexual dysfunction
Withdrawal: nausea, dizziness, anxiety, tremor, palpitations
INX:
Fluoxetine and paroxetine inhibit CYP2D6 (reduce TCA elimination)
Citalopram causes fewer drug INX
Serotonin Syndrome when given with MAO-I
Tremor, myoclonus, muscle rigidity, hyperthermia, and cardio collapse
Tx: Antiseizure drug, muscle relaxant, 5-HT blocker (cyproheptadine)
Fluoxetine should be d/c'd for 4-5 weeks before MAO-I given
MAO-I d/c'd 2 weeks before SSRI
Overdose:
Seizures (fluoxetine)
|
|
|
Term
|
Definition
Class: Selective Serotonin Reuptake Inhibitor (SSRI)
MOA:
Block 5-HT reuptake transporter in presynaptic terminals
Take two weeks for max benefit
Renal excretion except paroxetine and sertraline!
Fluoxetine has longest half life
Clinical uses:
Drug of choice for treatment of depression!
Generalized anxiety
Panic attacks
OCD (fluvoxamine)
Premenstrual dysphoric disorder- PMDD (fluoxetine and sertraline)
Bulimia (fluoxetine)
Side effects:
GI (n/v/d) most common
Sleep disturbances:
Paroxetine and fluvoxamine- sedating
Fluoxetine- activating
Sexual dysfunction
Withdrawal: nausea, dizziness, anxiety, tremor, palpitations
INX:
Fluoxetine and paroxetine inhibit CYP2D6 (reduce TCA elimination)
Citalopram causes fewer drug INX
Serotonin Syndrome when given with MAO-I
Tremor, myoclonus, muscle rigidity, hyperthermia, and cardio collapse
Tx: Antiseizure drug, muscle relaxant, 5-HT blocker (cyproheptadine)
Fluoxetine should be d/c'd for 4-5 weeks before MAO-I given
MAO-I d/c'd 2 weeks before SSRI
Overdose:
Seizures (fluoxetine)
|
|
|
Term
|
Definition
Class: Serotonin/Norepinephrine Reuptake Inhibitor (SNRI)
MOA:
Nonselective monoamine reuptake inhibitor
Don't take with food
Metabolized by CYP2D6 and CYP1A2
Highly bound to plasma protein
Clinical uses:
Tx major depressive disorder
Tx GAD
Tx neuropathic pain, diabetic neuropathy, and fibromyalgia (may work directly on pain pathway)
Stress urinary incontinence
Side effects:
GI: nausea, dry mouth, constipation
CNS (stimulatory and inhibitory): headache, insomnia, fatigue, somnolence, agitation
Sexual dysfunction
Dermatologic: hyperhidrosis, rash, pruritis
Sudden d/c --> seizure
INX:
Contra: MAO-I or uncontrolled narrow-angle glaucoma
CYP2D6 inhibitor: paroxetine
CYP1A2 inhibitor: fluvoxamine |
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Term
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Definition
Class: Serotonin/Norepinephrine Reuptake Inhibitor (SNRI)
MOA:
Nonselective monoamine reuptake inhibitor
Only inhibits NE reuptake at high doses
Also mildly inhibits dopamine reuptake
Hepatic metabolism
Renal excretion
Desvenlafaxine = active metabolite
Clinical uses:
Tx major depressive disorder
Tx GAD, social anxiety disorder, and panic disorder
Tx neuropathic pain, diabetic neuropathy, and fibromyalgia (may work directly on pain pathway)
Stress urinary incontinence
Side effects:
GI: nausea, dry mouth, anorexia, constipation
CNS (stimulatory and inhibitory): headache, insomnia, somnolence, dizziness, nervousness, asthenia
Sexual dysfunction
High doses: HTN
INX:
Contra: MAO-I
Inhibits metabolism of alprazolam, triazolam, and haloperidol |
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Term
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Definition
Class: Atypical Antidepressant
MOA:
Unknown- possibly affects NE or dopamine reuptake
Short half life
Clinical uses:
Major depressive disorder
Seasonal major depressive episodes
ADHD
Neuropathic disorder
Smoking cessation
PMDD
Side effects: Low!
Tremor
Insomnia
Agitation
Seizures (high dose)
Dry mouth
Sweating
Blurred vision |
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Term
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Definition
Class: Atypical antidepressant
MOA:
Block 5-HT2 and alpha-2 receptors
Presynaptic alpha-2 antagonist: increase monoamine release
Clinical uses:
Tx major depressive disorder
Side effects:
Autonomic effects d/t increased NE release
Sedating (block H1 receptor) - can be useful in patients with insomnia
Increased appetite and weight gain
INX:
Contra: MAO-I in past 2 weeks |
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Term
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Definition
Class: Atypical antidepressant
MOA:
Block 5-HT2A receptor and inhibit serotonin and NE transport
Clinical uses:
Depression (?)
Side effects:
Priapism
Weight gain
Sedating- H1 blocker |
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Term
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Definition
Class: Atypical antidepressant
MOA:
Block 5-HT2A receptor and inhibit serotonin and NE transport
Clinical uses:
Depression (?)
Side effects:
Hepatotoxic
Sedating- H1 blocker
INX:
Inhibit P450, therefore inhibit alprazolam and triazolam metabolism |
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Term
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Definition
Class: Atypical antidepressant
MOA:
Selective norepinephrine reuptake inhibitor
Clinical uses:
ADHD
Side effects:
Nausea
Appetite suppression
Sleep disturbance
Jitteriness
Irritability
Sexual dysfunction
Insomnia
INX:
Contra- MAO-I (2 weeks) and narrow angle glaucoma |
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