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Block 3 Pharm
PCSOM Block 3 Pharm
| 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) | (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) | (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) | (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) | (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 | 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) | Methamphetamine | increased alertness, decreased fatigue, decreased appetite | (blank) |
| CNS Stimulants - Amphetamine Derivative | 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 | 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) | (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) | (blank) |
| CNS Stimulants | alpha & beta adrenergic agonist; enhances release of NE | (blank) | OTC - energy booster - inhibit somnolence | Ephedrine | (blank) | (blank) |
| CNS Stimulants | Blocks reuptake of dopamine (also NE) by inhibiting dopamine transporter | (blank) | (blank) | Cocaine | (blank) | (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) | (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) | (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) | (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) | (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) | (blank) |
| Atypical Antidepressants - 2nd Generation | Inhibits neuronal uptake of dopamine & some NE | Seizures with alcohol | Depression & Mania | Bupropium | (blank) | (blank) |
| Atypical Antidepressants - 2nd Generation | Inhibits reuptake of serotonin | Sedation | Depression & Mania | Trazadone | (blank) | (blank) |
| Atypical Antidepressants - 2nd Generation | Antagonist at alpha2 adrenergic & histamine H1 receptors | Sedation; 1% incidence of agranulocytosis | Depression & Mania | Mirtazapine | (blank) | (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) | (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) | (blank) |
| Lithium Salts | Thought to alter cellular concentration of IP3 | low safety factor and therapeutic index | Bipolar Disorder | Lithium Salts | (blank) | (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) | (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) | (blank) |
| Anticonvulsants | Increase threshold for neuronal firing | depress cognitive performance, sedation, ataxia, vertigo, morbilliform rash | Febrile seizures in children | Phenobarbital | (blank) | (blank) |
| Anticonvulsants | Increase threshold for neuronal firing | depress cognitive performance, sedation, ataxia, vertigo, morbilliform rash | Antiepileptic | Primidone | (blank) | (blank) |
| Anticonvulsants | Produces small reductions of low threshold T Type Ca2+ currents | hyperammonemia, hepatotoxic | Myoclonic seizures | Valproic Acid | (blank) | (blank) |
| Anticonvulsants | large reductions of low threshold T Type Ca2+ currents | Eosinophilia | Absence Seizures | Ethosuximide | (blank) | (blank) |
| Benzo - Long Acting | GABA - Cl- complex | (blank) | DOC Myoclonic Seizures | Clonazepam | (blank) | (blank) |
| Benzo - long acting | GABA-Cl- complex | (blank) | DOC - Status epilepticus | Diazepam | (blank) | (blank) |
| Anticonvulsant | Carbonic anhydrase inhibitor | (blank) | Absence seizures | Acetazolamide | (blank) | (blank) |
| Anticonvulsant | Increase of GABA synthesis & release | (blank) | Adjunctive for partial seizures; pain management | Gabapentin | (blank) | (blank) |
| Anticonvulsants | Inhibits release of glutamate | (blank) | Adjunctive for treatment of partial seizures | Lamotrigine | (blank) | (blank) |
| Anticonvulsants | Blocks GABA uptake | (blank) | Adjunctive for treatment of partial seizures | Tiagabine | (blank) | (blank) |
| Anticonvulsants | Blocks glutamate receptors | renal stones | Adjunctive for treatment of partial seizures | Topiramate | (blank) | (blank) |
| Anticonvulsants | unknown | Dizziness, somnolence, fatigue, coordination difficulties | Adjunctive for treatment of partial seizures | Levetiracetam | (blank) | (blank) |
| Anticonvulsants | Increase inactive state of Na+ channels | Dizziness, somnolence, fatigue, coordination difficulties | Adjunctive and monotherapy for treatment of partial seizures | Oxcarbazepine | (blank) | (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) | (blank) |
| Anticonvulsants | Increase of GABA synthesis & release (greater than gabapentin) | Class V drug | Adjunctive for treatment of partial seizures; peripheral neuralgia | Pregabalin | (blank) | (blank) |
Created by:
spurrp