PCSOM Block 3 Pharm

Help!

Drug Class

Mech of Action

Side Effects

Indications for use

Drug

Advantages

Disadvantages

Benzo - Short Acting

Binding of BDZ enhances affinity of GABA, resulting in more freq opening of Cl channels, causing nerve hyperpolarization, resulting in inhibition of neuronal firing.

Drowsiness & confusion; Ataxia with high doses; cognitive impairment

Antianxiety

Oxazepam

Good choice for elderly and those with hepatic disease - no active metabolites

Tolerance; Dependence; Withdrawal

🗑

Benzo - Intermediate Acting

Binding of BDZ enhances affinity of GABA, resulting in more freq opening of Cl channels, causing nerve hyperpolarization, resulting in inhibition of neuronal firing.

Drowsiness & confusion; Ataxia with high doses; cognitive impairment

Antianxiety

Lorazepam

Good choice for elderly and those with hepatic disease - no active metabolites

Tolerance; Dependence; Withdrawal

🗑

Benzo - Intermediate Acting

Binding of BDZ enhances affinity of GABA, resulting in more freq opening of Cl channels, causing nerve hyperpolarization, resulting in inhibition of neuronal firing.

Drowsiness & confusion; Ataxia with high doses; cognitive impairment; Tolerance; Dependence; Withdrawal

Antianxiety Panic Disorder

Alprazolam

(blank)

Tolerance, Dependence, Withdrawal

🗑

Benzo - Long Acting

Binding of BDZ enhances affinity of GABA, resulting in more freq opening of Cl channels, causing nerve hyperpolarization, resulting in inhibition of neuronal firing.

Drowsiness & confusion; Ataxia with high doses; cognitive impairment; Tolerance; Dependence; Withdrawal

Antianxiety

Chlordiazepoxide

(blank)

Tolerance, Dependence, Withdrawal

🗑

Benzo - Long Acting

Binding of BDZ enhances affinity of GABA, resulting in more freq opening of Cl channels, causing nerve hyperpolarization, resulting in inhibition of neuronal firing.

Drowsiness & confusion; Ataxia with high doses; cognitive impairment; Tolerance; Dependence; Withdrawal

Antianxiety

Diazepam

(blank)

Tolerance, Dependence, Withdrawal

🗑

Benzo - Long Acting

Binding of BDZ enhances affinity of GABA, resulting in more freq opening of Cl channels, causing nerve hyperpolarization, resulting in inhibition of neuronal firing.

Drowsiness & confusion; Ataxia with high doses; cognitive impairment; Tolerance; Dependence; Withdrawal

Antianxiety

Clorazepate

(blank)

Tolerance, Dependence, Withdrawal

🗑

Azapirones

Partial agonist; actions mediated by 5-HT1A receptors; coupled to G proteins; increased opening of Cl channels; hyperpolarization of neuron; resulting in decreased firing.

headache & dizziness

Long term therapy of chronic anxiety

Buspirone

Good for pts with Hx of Substance Abuse

Slow onset of therapeutic action (about 2 wks)

🗑

SSRI

Inhibits reuptake of 5-HT at the transporter

CNS: insomnia, tremor; CV: palpitations, postural hypotension (paroxetine only), vasodilation; GI: N/V and diarrhea; GU: loss of libido & sexual dysfunction

Social anxiety disorder, Panic Disorder, Depression & Mania

Paroxetine

(blank)

Slow onset (about 2 wks); Drug Interactions with MAOI, TCA, Tryptophan, and Warfarin

🗑

SSRI

Inhibits reuptake of 5-HT at the transporter

CNS: insomnia, tremor; CV: palpitations, postural hypotension (paroxetine only), vasodilation; GI: N/V and diarrhea; GU: loss of libido & sexual dysfunction

PTSD, Panic Disorder, Depression & Mania

Sertraline

(blank)

Slow onset (about 2 wks); Drug Interactions with MAOI, TCA, Tryptophan, and Warfarin

🗑

Serotonin & NE Uptake Inhibitor

Blocks both serotoning & NE reuptake transporters

CNS: insomnia, tremor; CV: palpitations, postural hypotension (paroxetine only), hypertension, vasodilation; GI: N/V and diarrhea; GU: loss of libido & sexual dysfunction

General anxiety disorder

Venlafaxine

(blank)

DO NOT ABRUPTLY DISCONTINUE

🗑

Antihistamines

Antagonist at H1 receptors

Sedation

General Anxiety disorder

Hydroxyzine HCl

short acting

(blank)

🗑

Antihistamines

Antagonist at H1 receptors

Sedation

General Anxiety disorder

Hydroxyzine pamoate

long acting

(blank)

🗑

Typical Antipsychotic - Phenothiazines

Antagonism at presynaptic D2 & postsynaptic D2 receptors resulting in physiological depolarization inactivation.

Acute dystonia (diphenhydramine), akathisia, parkinsonism, Neuroleptic malignant syndrome (Dantrolene), Tardive dyskinesia (irreversible)

Schizophrenia

Chlorpromazine

(blank)

🗑

Typical Antipsychotic - Phenothiazines

Antagonism at presynaptic D2 & postsynaptic D2 receptors resulting in physiological depolarization inactivation.

Acute dystonia (diphenhydramine), akathisia, parkinsonism, Neuroleptic malignant syndrome (Dantrolene), Tardive dyskinesia (irreversible)

Schizophrenia

Trifluoperazine

(blank)

🗑

Typical Antipsychotic - Phenothiazines

Antagonism at presynaptic D2 & postsynaptic D2 receptors resulting in physiological depolarization inactivation.

Acute dystonia (diphenhydramine), akathisia, parkinsonism, Neuroleptic malignant syndrome (Dantrolene), Tardive dyskinesia (irreversible)

Schizophrenia

Fluphenazine

most potent

(blank)

🗑

Typical Antipsychotic - Phenothiazines

Antagonism at presynaptic D2 & postsynaptic D2 receptors resulting in physiological depolarization inactivation.

Acute dystonia (diphenhydramine), akathisia, parkinsonism, Neuroleptic malignant syndrome (Dantrolene), Tardive dyskinesia (irreversible)

Schizophrenia

Thioridazine

(blank)

🗑

Typical Antipsychotic - Butyrophenones

Antagonism at presynaptic D2 & postsynaptic D2 receptors resulting in physiological depolarization inactivation.

Acute dystonia (diphenhydramine), akathisia, parkinsonism, Neuroleptic malignant syndrome (Dantrolene), Tardive dyskinesia (irreversible)

Schizophrenia

Haloperidol

very potent

(blank)

🗑

Typical Antipsychotic - Thioxanthenes

Antagonism at presynaptic D2 & postsynaptic D2 receptors resulting in physiological depolarization inactivation.

Acute dystonia (diphenhydramine), akathisia, parkinsonism, Neuroleptic malignant syndrome (Dantrolene), Tardive dyskinesia (irreversible)

Schizophrenia

Thiothixene

(blank)

🗑

Atypical Antipsychotic

High affinity for dopamine D4 receptors

Severe agranulocytosis

Schizophrenia

Clozapine

Intermediate autonomic effects

(blank)

🗑

Atypical Antipsychotic

High affinity for 5-HT2 receptor

Increases QT wave - do not use in CV disease

Schizophrenia

Risperidone

Low risk of causing Extrapyramidal symptoms; minimal sedation

(blank)

🗑

Atypical Antipsychotic

High affinity for 5-HT2 receptor

(blank)

Schizophrenia

Olanzapine

No QT effect, Low EPS profile, minimal sedation, ONLY ANTIPSYCHOTIC that lessens effects of tardive dyskinesia

(blank)

🗑

Atypical Antipsychotic

High affinity for 5-HT2 receptor

(blank)

Schizophrenia

Quetiapine

Low risk of causing Extrapyramidal symptoms; minimal sedation; no QT effect

(blank)

🗑

CNS Stimulants - Methylxanthines

Inhibits PDE resulting in increased cAMP AND is an antagonist at adenosine A1 & A2 receptors causing an increase in neurotransmission by amplifying the cyclic nucleotide 2nd msgr cascade

Doses >200mg produces nervousness, restlessness & tremors; N/V

Stimulant

Caffeine (coffee & cola-flavored drinks)

Increased Alertness, loss of fatigue,Stimulation of respiration, sustained attention

(blank)

🗑

CNS Stimulants - Methylxanthines

Inhibits PDE resulting in increased cAMP AND is an antagonist at adenosine A1 & A2 receptors causing an increase in neurotransmission by amplifying the cyclic nucleotide 2nd msgr cascade

N/V, very high doses - seizures that are refractory to anticonvulsant drugs

Stimulant

Theophylline

Stimulates respiration

(blank)

🗑

CNS Stimulants

stimulate nicotinic receptors in CNS, depolarization, euphoria & arousal

(blank)

Smoking cessation

Nicotine

Improves attention, learning, problem solving & reaction time

(blank)

🗑

CNS Stimulants - Amphetamines

Release of biogenic amines (NE, Dop, & 5HT) from storage in nerve terminals

High abuse potential, tolerance, dependence, insomnia, tenseness, irritability, weakness, confusion, delirium, paranoid hallucinations, suicidal/homicidal tendencies, headache, palpitations, arrhythmias, HTN, excessive sweating, circulatory collapse

(blank)

Dextroamphetamine

increased alertness, decreased fatigue, decreased appetite

(blank)

🗑

CNS Stimulants - Amphetamines

Release of biogenic amines (NE, Dop, & 5HT) from storage in nerve terminals

(blank)

Methamphetamine

increased alertness, decreased fatigue, decreased appetite

(blank)

🗑

CNS Stimulants - Amphetamine Derivative

Release of biogenic amines (NE, Dop, & 5HT) from storage in nerve terminals

Narcolepsy & ADHD

Methylphenidate

increased alertness, decreased fatigue, decreased appetite

Safety Concerns

🗑

CNS Stimulants - Amphetamine Derivative

Dissimilar to methylphenidate but elecits similar changes with minimal effects on CV

(blank)

Narcolepsy & ADHD

Pemoline

(blank)

🗑

CNS Stimulants - Amphetamine Derivative

(blank)

CONTRAINDICATED in pts with Hx of CV problems; HTN crisis with MAOI

Adjunct to behavioral modification (3 weeks only)

Phentermine

(blank)

🗑

CNS Stimulants

alpha & beta adrenergic agonist; enhances release of NE

(blank)

OTC - energy booster - inhibit somnolence

Ephedrine

(blank)

🗑

CNS Stimulants

Blocks reuptake of dopamine (also NE) by inhibiting dopamine transporter

(blank)

Cocaine

(blank)

🗑

CNS Stimulant

Regulate normal wakefulness or decreases GABA firing

anxiety & depression

Narcolepsy

Modafinil

wakefulness without generalized stimulation; Not a direct or indirect acting dopamine receptor agonist; no effect on BP; minimal locomotor activity

(blank)

🗑

CNS Stimulant

Not understood

Depression, Bedwetting, Sleep walking; Abuse potential

Narcolepsy

Sodium Oxybate

Reduces number of cataplexy attacks

High abuse potential

🗑

Tricyclic Antidepressant

Potentiates NE & 5-HT by inhibiting transport to reuptake

ANS effects, Muscarinic cholinergic antagonism; CV effects; Sedation; Narrow therapeutic index; weight gain, Interacts with MAOI & Ethanol

Depression & Mania

Imipramine

(blank)

🗑

Tricyclic Antidepressant

Potentiates NE & 5-HT by inhibiting transport to reuptake

ANS effects, Muscarinic cholinergic antagonism; CV effects; Sedation; Narrow therapeutic index; weight gain, Interacts with MAOI & Ethanol

Depression & Mania

Amitriptyline

(blank)

🗑

SSRI

Inhibits reuptake of 5-HT at transporter

CNS: insomnia, tremor; CV: palpitations, postural hypotension (paroxetine only), vasodilation; GI: N/V and diarrhea; GU: loss of libido & sexual dysfunction

Depression & Mania

Citalopram

(blank)

🗑

SSRI

Inhibits reuptake of 5-HT at transporter

CNS: insomnia, tremor; CV: palpitations, postural hypotension (paroxetine only), vasodilation; GI: N/V and diarrhea; GU: loss of libido & sexual dysfunction

Depression & Mania

Escitalopram

(blank)

🗑

SSRI

Inhibits reuptake of 5-HT at transporter

CNS: insomnia, tremor; CV: palpitations, postural hypotension (paroxetine only), vasodilation; GI: N/V and diarrhea; GU: loss of libido & sexual dysfunction

Depression & Mania

Fluoxetine

(blank)

🗑

Atypical Antidepressants - 2nd Generation

Inhibits neuronal uptake of dopamine & some NE

Seizures with alcohol

Depression & Mania

Bupropium

(blank)

🗑

Atypical Antidepressants - 2nd Generation

Inhibits reuptake of serotonin

Sedation

Depression & Mania

Trazadone

(blank)

🗑

Atypical Antidepressants - 2nd Generation

Antagonist at alpha2 adrenergic & histamine H1 receptors

Sedation; 1% incidence of agranulocytosis

Depression & Mania

Mirtazapine

(blank)

🗑

MAOI

site-directed, irreversible inhibitors that regulate metabolic degradation NE, 5-HT, and Dopamine

Drowsiness, orthostatic hypotension, blurred vision, dryness of mouth, dysuria, constipation, Interacts with everything

Depression and Mania

Tranylcypromine

(blank)

🗑

MAOI

site-directed, irreversible inhibitors that regulate metabolic degradation NE, 5-HT, and Dopamine

Drowsiness, orthostatic hypotension, blurred vision, dryness of mouth, dysuria, constipation, Interacts with everything

Depression and Mania

Phenelzine

(blank)

🗑

Lithium Salts

Thought to alter cellular concentration of IP3

low safety factor and therapeutic index

Bipolar Disorder

Lithium Salts

(blank)

🗑

Anticonvulsants

Decreased Na+ influx into neuron by prolonging inactivated state

Gingival hyperplasia, coarsening of facial features, hirsutism, antiarrhythmic effect, fetal hydantoin syndrome

Tonic-Clonic seizures, Partial seizures

Phenytoin

(blank)

🗑

Anticonvulsants

Decreased Na+ influx into neuron by prolonging inactivated state

Aplastic anemia, agranulocytosis, thrombocytopenia, potential for inducing serious liver disease

tonic-clonic seizures, partial seizures

Carbamazepine

(blank)

🗑

Anticonvulsants

Increase threshold for neuronal firing

depress cognitive performance, sedation, ataxia, vertigo, morbilliform rash

Febrile seizures in children

Phenobarbital

(blank)

🗑

Anticonvulsants

Increase threshold for neuronal firing

depress cognitive performance, sedation, ataxia, vertigo, morbilliform rash

Antiepileptic

Primidone

(blank)

🗑

Anticonvulsants

Produces small reductions of low threshold T Type Ca2+ currents

hyperammonemia, hepatotoxic

Myoclonic seizures

Valproic Acid

(blank)

🗑

Anticonvulsants

large reductions of low threshold T Type Ca2+ currents

Eosinophilia

Absence Seizures

Ethosuximide

(blank)

🗑

Benzo - Long Acting

GABA - Cl- complex

(blank)

DOC Myoclonic Seizures

Clonazepam

(blank)

🗑

Benzo - long acting

GABA-Cl- complex

(blank)

DOC - Status epilepticus

Diazepam

(blank)

🗑

Anticonvulsant

Carbonic anhydrase inhibitor

(blank)

Absence seizures

Acetazolamide

(blank)

🗑

Anticonvulsant

Increase of GABA synthesis & release

(blank)

Adjunctive for partial seizures; pain management

Gabapentin

(blank)

🗑

Anticonvulsants

Inhibits release of glutamate

(blank)

Adjunctive for treatment of partial seizures

Lamotrigine

(blank)

🗑

Anticonvulsants

Blocks GABA uptake

(blank)

Adjunctive for treatment of partial seizures

Tiagabine

(blank)

🗑

Anticonvulsants

Blocks glutamate receptors

renal stones

Adjunctive for treatment of partial seizures

Topiramate

(blank)

🗑

Anticonvulsants

unknown

Dizziness, somnolence, fatigue, coordination difficulties

Adjunctive for treatment of partial seizures

Levetiracetam

(blank)

🗑

Anticonvulsants

Increase inactive state of Na+ channels

Dizziness, somnolence, fatigue, coordination difficulties

Adjunctive and monotherapy for treatment of partial seizures

Oxcarbazepine

(blank)

🗑

Anticonvulsants

Inhibits T type Ca2+ currents

Is a sulfonamide - don't give to pts allergic to sulfa drugs

Adjunctive for treatment of partial seizures

Zonisamide

(blank)

🗑

Anticonvulsants

Increase of GABA synthesis & release (greater than gabapentin)

Class V drug

Adjunctive for treatment of partial seizures; peripheral neuralgia

Pregabalin

(blank)

🗑

Review the information in the table. When you are ready to quiz yourself you can hide individual columns or the entire table. Then you can click on the empty cells to reveal the answer. Try to recall what will be displayed before clicking the empty cell.

To hide a column, click on the column name.

To hide the entire table, click on the "Hide All" button.

You may also shuffle the rows of the table by clicking on the "Shuffle" button.

Or sort by any of the columns using the down arrow next to any column heading.
If you know all the data on any row, you can temporarily remove it by tapping the trash can to the right of the row.

Embed Code - If you would like this activity on your web page, copy the script below and paste it into your web page.

Normal Size Small Size show me how

Created by: spurrp