CNS Drugs Flashcards
1
Q
Zolpidem
A
Z-Drug. Commonly associated with sleep related behaviors. Short duration of action.
2
Q
Atomoxetine Indications
A
ADHD. Especially in addicts (doesn’t cause euphoria).
3
Q
Parkinson’s Pathophysiology
A
Caused by a loss of DA neurons in the nigrostriatal system. Treatment must balance Ach and DA.
4
Q
Cholinesterase Inhibitors MOA
A
Increase Ach in the nerve terminals. May slow the progression of Alzheimer’s.
5
Q
Mepivacaine
A
Amide LA. Intermediate duration of action.
6
Q
Eszopiclone
A
Z-Drug. Long half life. Used for long-term treatment.
7
Q
Secobarbital
A
Barbituate
8
Q
Smoking Cessation
A
Bupropion will treat nicotine craving.
9
Q
DOC for Bipolar Disorder
A
Lithium
10
Q
TCA MOA
A
Inhibit re-uptake of NE and 5HT. Also blocks alpha, histamine and Ach receptors. Dirty drugs!
11
Q
Galantamine
A
Cholinesterase Inhibitor used in Alzheimer’s
12
Q
Tigabine Indications
A
Adjunct for partial seizures.
13
Q
Metratazpine MOA
A
Blocks presynaptic alpha 2 receptors. Increases the release of NE and 5HT.
14
Q
Citalopram.
A
SSRI. DOC for depression. Low incidence of drug interactions.
15
Q
Z-Drugs MOA
A
Sedative-hypnotics. Bind the GABA receptor to increase GABA mediated inhibition.
16
Q
Alcohol MOA
A
Binds to GABAa receptrs to increase Cl influx and enhance GABA (inhibitory) transmisison. Increases beta-endorphins in the mesolimbic pathway.
17
Q
Cocaine effects
A
CNS stimulant. Increased SNS tone. Alertness, euphoria, hyperactivity, tachycardia, vasoconstriction, HTN, hyperprexia.
18
Q
Midazolam
A
Very short-acting Benzodiazepine. Used for anxiety disorders and short surgical procedures as anesthesia.
19
Q
DOC for Partial Seizures
A
Carbamazepine
20
Q
Vigabatrin Indications
A
Refractory complex partial seizures. West’s syndrome.
21
Q
Carbamazepine Indications
A
DOC for partial seizures. Also used for Trigeminal neuralgia, TC seizures and Refractory cases of Bipolar disorder.
22
Q
Disulfuram (antabuse) MOA
A
Inhibits aldehyde dehydrogenase. Causes build up of acetyldehyde (flusing, nausea, HA).
23
Q
Ropinirole
A
DA D2 agonist. Used as monotherapy in mild Parkinson’s. Can cause sudden sleep during the day.
24
Q
Korsakoff’s psychosis
A
Chronic disabling memory loss
25
Memantine
NMDA receptor antagonist, reduces excitotoxic effects of glutamate and slows degerneration. Used in the late stages of Alzheimer's in combination with a Cholinesterase Inhibitor.
26
Lamotrigine Indications
Partial seizures, Bipolar Disorder (prevents relapse). May be effective at treating myoclonic and absence seizures in children.
27
Carbamazepine SE
Diplopia, ataxia, high risk of SJS, Teratogenic.
28
Valproic Acid Indications
Second line treatment of absence seizures. Myoclonic seizures, bipolar disorder (rapid cycling), Migraine prophyaxis, mixed seizures.
29
Levodopa (L-dopa) Contraindications
Psychosis, Cardiac disease, malignant melanoma. Don'r use with MAOIs (HTN crisis).
30
Pramipexole
DA D2 agonist. Used as monotherapy in mild Parkinson's. Can cause sudden sleep during the day.
31
Olanzapine (Zyprexa)
Atypical Antipsychotic. Can also be used in bipolar disorder. Similar to clozapine without the risk of agranulocytosis. EPS is very rare. Contraindicated in DM due to hyperglycemia.
32
PCP/Ketamine
NMDA receptor antagonists. Developed as general dissociative anesthetics. Cause analgesia accompanied by aggression. Often produces psychosis (treat with haloperidol).
33
Botulinum Toxin
Direct acting muscle relaxant. Inhibits Ach release from the nerve at the junction. Very toxic in large amounts.
34
Amitriptyline
TCA. Tertiary amine (primarily 5HT uptake).
35
Nigrostriatal DA Pathway
SN to the Striaturm. Motor. Parkinson's (not enough DA) and the side effects of many antipsychotics.
36
Naltrexone Indications
Treatment of alcoholism and opiod addiction. Decreases craving.
37
Baclofen SE
Drowsiness, weakness. Respiratory depression with intrathecal administration (can reduce other SE and increase treatment).
38
Topiramate Indications
Partial and TC seizures. Migraine prevention.
39
Opiod MOA
Closes voltage gated Ca channels on presynaptic nerve terminals to decrease neurotransmitter release and neuronal activity. Decreases glutamate from the dorsal horn or the spinal cord to the brain. Mu receptors also open K channels to hyperpolarize the cell.
40
Alcohol Withdrawal Treatment
Hydration. Diazepam or chlordiazepoxide to prevent seizures/DTs. Lorazepam to treat seizures. Phenytoin is second line to treat seizures.
41
Pentazocine MOA
Mixed Opiod. Kappa agonist (dysphoria) and partial Mu agonist.
42
DOC for Depression
Citalopram
43
Topiramate MOA
Anti-convulsant. Blocks Na channels to potentiate GABA and block glutamate.
44
SNRI Indications
Depression, neuro pain, post menopausal hot flashes. Have more side effects than SSRIs.
45
Buproprion Contraindications
History of seizures.
46
Dantrolene
Direct acting Muscle Relaxant. Inhibits Ca release by blocking the RyR1 channel on the SR (interferes with excitation/contraction coupling). Used in neuroleptic malignant syndrome and malignant hyperthermia.
47
Vigabatrin SE
Visual field problems and retinal damage.
48
Gabapentin Indications
Adjunct use for partial and TC seizures. Neuropathic pain and Bipolar Disorder (rapid cycling).
49
Clonazepam MOA
Benzodiazapine. Stimulates GABA.
50
Ethosuximide Indications
DOC for absence seizures.
51
Buproprion Indications
Refractory depression (combined with SSRIs), ADHD, Alcoholism, smoking cessation (extended release). Causes less sexual dysfunction than the other antidepressants.
52
Trazodone Indications
Sleep aid and pain. Not useful in depression.
53
Amantadine
Antiviral that increases DA transmissioin and is used to treat early/mild cases of parkinson's or as an adjunct to other treatment . Can cause livedo reticularis (red/blue spotting of skin).
54
Imipramine
TCA. Tertiary amine (primarily 5HT).
55
Oxymorphone
Moderate Opiod. Similar to oxycodone but doesn't need to be activated by CYP2D6.
56
GHB
GABA receptor weak agonist. Developed as general dissociative anesthetics. Used as date rape drugs.
57
Carbamazepine MOA
Anticonvulsant. Blocks Na channels (decreases glutamate)
58
Amide Metabolism
Metabolized via CYP 450s. Can cause toxicity in patients with liver disease. Excreted by the kidneys.
59
PTSD Treatment
Anti-Depressants
60
Atomoxetine MOA
Selective NE reuptake inhibitor.
61
Gabapentin MOA
Anti-convulsant. GABA analogue.
62
Phenytoin/Fosphenytoin SE
Gingival hyperplasia. Risk of SJS. Teratogenicity.
63
Methanol Poisoning Treatment
Fomepizole (alcohol dehydrogenase inhibitor) can also use ethanol.
64
Meperidien (demerol) SE
Renal failure (don't use longer than 48 hours), Seizures (due to metabolite normeperidine), Tachycardia. MAOI: serotonin syndrome. No antitussive effects.
65
Antipsychotic Drug Interactions
Sedative-Hypnotics: Increased Sedation Smoking: Induces CYP450s
66
Naltrexone MOA
Opiod receptor antagonist. Reduces craving. Long-acting.
67
SNRI MOA
Inhibits NE and 5HT reuptake
68
Fluphenazine
Classical Antipsychotic. Selective for DA D2 receptors. Less anticholinergic effects so higher risk of EPS.
69
Meperidien (demerol) MOA
Opiod. Mu agonist plus NE/5HT reuptake inhibitor. Also blocks muscarinic receptors.
70
Diazepam
Long- acting Benzodiazepine. Used in anxiety disorders, status epilepticus, alcohol/barbituate withdrawal (prevents seizures) and as a muscle relaxant
71
Ester Metabolism
Metabolized via butyrulcholinesterases in the plasma. Shorter duration of action and increased systemic toxicity. excreted by the kidneys. Has PABA as a metabolite which can cause allergic reactions.
72
Donepezil
Cholinesterase Inhibitor used in Alzheimer's
73
Levetricetam SE
Dizziness, ataxia, asthenia (weakness), minimal drug interactions.
74
Hydromorphone
Strong opiod
75
Morphine
Strong Opiod. Severe pain. Injected. Associated with itching and vomiting.
76
Trazodone MOA
Anti-depressant. 5HT receptor antagonist.
77
Chlorpromazine MOA
Classical antipsychotic. Blocks DA D2 receptors but also alpha adrenergic and Ach receptors.
78
Rasagiline SE
Causes insomnia (take in the morning). Don't use with Merperidine (stupor, rigidity, agitation) or TCA/SSRIs (serotonin syndrome).
79
Benzocaine
Ester LA. Topical use only. Pka=3.5 so always in nonionized form.
80
Acute Alcohol Toxicity Presentation
Emesis, stupor, coma, respiratory depression, electrolyte imbalances, hypothermia, decreased BP and CO.
81
Diazepam MOA
Centrally acting muslce relaxant (benzodiazepine). GABAa medicated presynaptic inhibition of the spinal cord. Also used in anxiety disorders, status epilepticus, alcohol/barbituate withdrawal (prevents seizures)
82
Tramadol Drug interactions
Serotonin syndrome if combined with MAOIs, TCAs, SSRIs/ Seizures: antidepressants.
83
Barbituates SE
Low margin of safety! Drowsiness, respiratory depression. Paradoxical excitement. Causes euphoria (drug of abuse) Supra-additive effect with alcohol.
84
Methamphetamines
Increases the release of DA and NE in the basal ganglia.. Rapid physical and psychological dependence. Cardiac toxicity, odor (hyperthermia), meth mouth, meth bugs.
85
Lithium MOA
Suppresses second messengers. Not metabolized. Excreted by the kidneys.
86
Fluoxetine
SSRI. Inhibits CYP450 (drug interactions). Inhibits conversion of codeine to morphine. Impairs BGL in DM.
87
D2 agonist Side effects
Anorexia, N/V, GI upset, Dyskinesias, mental disturbance, decreased prolactin.
88
Thopental
Barbituate. Used for induction of anesthesia.
89
SSRI Drug Interactions
MAOIs: Serotonin syndrome St. Johns Wort: Serotonin syndrome Opiods: Fluoxetine inhibits the conversion of codeine to morphine. Tramadol: inhibits 5HT reuptake and can lead to seizures and serotonin syndrome.
90
Nitrous Oxide
Used as an inhalant. Chronic use causes peripheral neuropathy. Frequently abused by dentists.
91
Classic Antipsychotics MOA
"neuroleptics." Block DA D2 receptors. Target the mesolimbic system so only alleviates positive symptoms.
92
Mesolimbic DA Pathway
From the VTA to the Limbic system. Emotion. Too much DA causes the positive symptoms of schizophrenia.
93
Cocaine overdose
V-tach and V-fib. Strokes, bleed, seizures.
94
Pentazocine Indications
Moderate pain. Useful in addicts (low abuse potential).
95
Fetal Alcohol syndrome
microceophaly, mental retardation, poor coordination, flat face, joint abnormalities, heart defects, impaired immune system.
96
Apomorphone
DA D2 agonist. Used as "rescue" for the on/off phenomenon in successful L-dopa therapy. Caused N/V give antiemetic (trimethobrinzamide) beforehand.
97
Metratazpine Indications
None of the side effects associated with SSRIs (blocks 5HT in other places). Useful in depression mixed with insomnia or anxiety.
98
Methadone Indications
Treatment for addicts (prevent withdrawal) and long term pain control.
99
Phenelzine
MAOI. Inhibits MAO-A and MAO-B. Drug of last choice for depression. Don't eat dietary tyramine (HTN crisis).
100
Lidocaine
Amide LA. Rapid onset. Used for infiltrative and epidural blocks. Not for spinal blocks (risk of TNS). Also used as an anti arrhythmic.
101
Venlaxfaxine
SNRI. May increase BP.
102
Development of Opiod Tolerance
Occurs rapidly. NMDA antagonists may decrease the development of tolerance. No tolerance develops to miosis, constipation or seizures.
103
Ethosuximide MOA
Anti-convulsant. Inhibits T-type Ca channels
104
Pharmacokinetic Alcohol Tolerance
Increased Alcohol metabolism because CYP2E1 is induced.
105
Benzodiazepines and Alcohol
Supra additive effect.
106
SSRI MOA
Selectively inhibit 5HT reuptake. Takes 2-3 weeks to have effects.
107
Dextromethorphan MOA
Antitussive Opiod. Blocks NMDA and decreases 5HT reuptake.
108
Dextromethorphan Indications
Cough suppression. Don't' use with MAOIs (serotonin syndrome)
109
Levodopa (L-dopa) SE
Has peripheral effects of N/V. Effectiveness will decrease over time. Has no effect on progression.
110
Benzodiazepines MOA
CNS depressant. GABAa agonist and increases the affinity for GABA (needs GABA) has ceiling effect.
111
Methadone MOA
Opiod. Strong mu agonist that also blocks NMDA and NE/5HT reuptake. Long duration of action. Decreased tolerance.
112
Cholinesterase Inhibitors SE
N/V, diarrhea, stomach cramps.
113
Desipramine
TCA. Secondary amine (primarily NE)
114
Duloxetine
SNRI. Hepatotoxicity.
115
Quetiapine (Seroquel)
Atypical Antipsychotic. Used to promote sleep and for sleep maintenance. Similar to clozapine without risk of agranulocytosis. Very sedating. Does not elevate prolactin levels.
116
SSRI SE
Mild compared to the TCAs. GI, weight change, CNS stimulation, Sexual dysfunction.
117
Ramelteon Indications
Resets sleep-wake cycle. Good for use in addicts.
118
Valproic Acid MOA
Anti-convulsant. Blocks Ca channels, Na channels, and may enhance GABA activity.
119
Cocaine as LA
Ester LA. Inhibits Na channels secondary to effects on increases DA in the CNS. Used topically. Decreases dental bleeding.
120
Clonazepam Indications
Absence and myoclonic seizures. West's syndrome.
121
Levodopa (L-dopa) Indications
Treats Parkinson's by improving bradykinesia for the first 3-4 years.
122
Effects of Opiods
Analgesia (develop tolerance), sedation, euphoria or dysphoria, histamine release (itching), emesis (esp. morphine), Antitussive (codeine and dextromethorphan), respiratory depression (useful in pulmonary edema), elevated intracranial pressure, Miosis (no tolerance), truncal rigidity (fentanyl), CONSTIPATION (no tolerance) Difficulty urinating.
123
Z-Drugs Indications
Insomia. Sedation with no anxiolytic, anticonvulsant or muscle relaxant properties.
124
Phenytoin/Fosphenytoin MOA
Anticonvulsants. Prolongs inactivation of Na channels (decreases glutamate).
125
Nalaxone
Opiod antagonist. Short duration of action. DOC for opiod overdose. Inject until pupils dilate.
126
Benzodiazepines Contraindications
Eldery, Sleep apnea, Pregnancy. Avoid abrupt withdrawla (rebound insomnia/anxiety).
127
Topiramate SE
Acute myopia and glaucoma.
128
Alprazolam
Intermediate-acting Benzodiazepine.
129
Phenobarbital
Barbituate. Anticonvulsant (partial seizures and TC seizures). HUGE Inducer CYP 450s.
130
Ramelteon MOA
Sedative-hypnotic. Melatonin analogue. No GABA effect.
131
Pentobarbital
Barbituate
132
Aripiprazole (Abilify) SE
Decreased esophageal motility. Low risk of EPS.
133
Carisoprodol
Acute local muscle relaxant. Metabolized to meprobamate (similar to barbituates) drug of abuse (caution in addicts).
134
Z-Drugs SE
Large margin of safety. Sleep related behaviors. Elderly may have confusion/memory loss. Rebound insomnia with abrupt withdrawal.
135
Entacapone
COMT inhibitor. Inhibits DA and L-dopa metabolism. Increases the pool of L-dopa available for the drain. Causes an orange color in the urine.
136
Acamprosate Indications
Treatment of Alcoholism. Decreases craving without liver toxicity.
137
MAOIs SE
Orthostatic hypotension, weight gain, insomnia.
138
Risperidone (Risperdal)
Atypical Antipsychotic. First line for psychosis. EPS and TD are rare.
139
Nortriptyline
TCA. Secondary amine (primarily NE)
140
Codeine MOA
Antitussive opiod. Has to be metabolized by CYP2D6 and converted into morphine.
141
Flumazenil Indications
Reverses effects of Benzodiazepine. Especially used to reverse Midazolam in surgical procedures.
142
DOC for absence seizures
Ethosuximide
143
DOC for Status Epilepticus
Diazepam
144
Clozapine
Atypical Antipsychotic. Last to choose due to the risk of agranulocytosis (have to monitor CBC closely). EPS and TD are very rare.
145
Ropivacaine
Amide LA. Long duration of action. S-enantiomer of bupivacaine (better clearance and less cardiac issues). Causes vasoconstriction.
146
Tuberoinfundibular DA Pathway
The hypothalamus to the pituitary (prolactin). Causes the side effects of many antipsychotics.
147
TCA Drug Interactions
Metabolized by CYP2D6 MAOIs: Serotonin Syndrome. Potentiate the sedative effects of alcohol and CNS depressants. Potentiate anticholinergic drug effects.
148
Alcohol Metabolism
Zero order (Rate is independent of concentration). Alcohol dehydrogenase is major enzyme. Secondary: MEOS and CYP2E1 (increases Acetaminophen toxicity), Induced with chronic consumption.
149
Selegiline
MAOI. Only inhibits MAO-B. Increases DA in the brain. Used in Parkinson's disease.
150
DOC for Anxiety
Benzodiazepines
151
Rivastigmine
Cholinesterase Inhibitor used in Alzheimer's
152
Lamotrigine Drug Interactions
Half life if DOUBLED with valproic acid.
153
Procaine
Ester LA. Short duration of action. Used for diagnostic nerve blocks.
154
Ethosuximide SE
Hiccups, SJS.
155
Fosphenytoin
Injectable version of phenytoin.
156
Temazepam
Benzodiazepine. Used for anxiety disorders and insomnia.
157
Tizanidine
Centrally acting muscle relaxant. Alpha 2 receptor agonist. Used for muscle spasm with limited muscle weakness. Very sedating.
158
Acamprosate MOA
Structural analogue of GABA. Restores balance between GABA and Glutamate.
159
Metratazpine SE
Blocks histamine (drowsiness).
160
Bupivacaine
Amide LA. Long duration of action. Used as epidural for labor/delivery. More potent sensory than motor block. High cardiotoxicity
161
Rasagiline MOA
MAOI that inhibits DA metabolism especially by MAO-B in the CNS to increase DA in the striatal pathway.
162
MAOIs MOA
Irreversibly inhibit MAO which metabolizes NE, DA and 5HT. MAO-A is in the CNS and periphery. MAO-B selectively metabolizes DA in the CNS.
163
Levetricetam Indications
Partial and TC seizures. Also used for myoclonic seizures.
164
Extrapyrimidal Symptoms (EPS)
Common side effect of antipsychotics (primarily classical). Due to blocking of the nigrostriatal DA pathway. Parkinson's like side effects (tremor, dyskinesia, rigidity). Treat with an anticholinergic like benztropine to correct the imbalance of DA and Ach.
165
MAOI Drug interactions
Serotonin syndrome with: meperidine, dextromethorphan, TCAs, SSRIs. Tramadol: Hyperpyrexia OTC cold meds (sympathomimetics): Severe HTN
166
Alzheimer's Pathophysiology
Degeneration of cholinergic neaurons. Beta-amyloid plaques and tau proteins.
167
Trihexyphenidyl
Muscarinic receptor antagonist, restores Ach and DA balance. Used as an adjunct to improve rigidity and tremor.
168
Cocaine MOA
Inhibits DA reuptake and secondarily inhibits Na channels.
169
Lamotrigine MOA
Anti-convulsant. Inactivation of Na channels.
170
Baclofen MOA
Centrally acting muscle relaxant. GABAb agonist (opens K channels causing hyperpolarization) and decreases presynaptic Ca influx (decreases neurotransmitter release).
171
Tigabine MOA
Anti-convulsant. Inhibits the reuptake of GABA via GAT1. Short half life. Few drug interactions.
172
DOC for restless leg syndrome
Ropinirole
173
Reward Pathway
Mesolimbic DA pathway. VTA to the NAc to the prefrontal cortex. All drugs of abuse release DA in the accumbens.
174
Buprenorphine Indications
Maintenance treatment of opiod addiction (decreases cravings).
175
Effects of Alcohol
CNS: disinhibition, mild euphoria, depressant and sedation. Smooth Muscle: Vasodilation (hypothermia) Heart: Depression of myocardial contractility Kidney: Decreases ADH (Diuresis).
176
Lorazepam
Intermediate-acting Benzodiazepine. Used for anxiety disorders and status epilepticus.
177
Barbituate Overdose and Treatment
Coma, respiratory depression. Treated by supportive care and alkalizing the urine. Don't use stimulants.
178
Pharmacodynamic Alcohol Tolerance
Down- regulation of GABA receptors and Up-regulation of NMDA receptors (blackout amnesia). Causes Withdrawal symptoms.
179
LSD
Act on 5HT receptors in the brain. Doesn't cause addiction. Euphoria, visual hallucinations, synesthesia.
180
Trazodone SE
Sedations, priapism, liver failure.
181
Bath Salts
Synthetic Cannabinoid agonist. Has psychoactive properties. Elevated HR and BP.
182
Flurazepam
Long-acting Benzodiazepine. Used for anxiety disorders, alcohol/barbituate withdrawal and insomnia.
183
Prochlorpromazine
Classical antipsychotic. Same as Chlorpromazine. Used as an antiemetic.
184
Tramadol MOA
Moderate Opiod. Weak mu agonist. Inhibits NE/5HT reuptake.
185
Parkinson's Presentation
Bradykinesia (slow movement), Muscle rigidity, resting tremors, impairment of posture balance and gait.
186
Cocaine long term side effects
Overall reduction in brain activity. Sever craving. Physical and physiological dependence.
187
Etidocaine
Amide LA. Intermediate duration of action. Inverse differential block (causes motor block before or even without sensory block).
188
Hydrocodone
Moderate Opiod. Activated by CYP2D6 (variable metabolizers.
189
Buspirone Indications
Relieves anxiety with no sedation. Good to use in addicts.
190
Flumazenil Contraindications
History of seizures or chronic alcohol abuse.
191
Paroxetine
SSRI. Used for OCD and Social Anxiety.
192
Flumazenil MOA
Benzodiazepine antagonist
193
Neuroleptic Malignant Syndrome (NMS)
Life threatening side effect. Muscle rigidity, hyperprexia. Caused by blockade of DA D2 receptors in the striatum and hypothalamus. Treat with dantrolene.
194
Ziprisadone (Geodon)
Atypical Antipsychotic. Used for tourette's and acute mania. Prolongs QT interval and causes sedation.
195
Nicotine
Activates nicotinic receptors in the CNS increases 5HT and DA. Intense psychological and physical dependence. Induces CYP450s.
196
Fentanyl
Strong, very potent opiod. Used in short surgical procedures. Truncal rigidity (rapid IV).
197
Levetricetam MOA
Anti-convulsant. Binds synaptic vsicular protein (SV2A) to decrease glutamate and increase GABA release.
198
Lithium SE
Diabetes insipidus. Small therapeutic window (Extremely toxic in overdose).
199
Chlordiazepoxide
Long-acting Benzodiazepine. Used in anxiety disorders and alcohol/barbituate withdrawal (prevent seizures).
200
Amphetamine MOA
Increase release of DA by reversing DA transport through the DAT.
201
Effect of Chronic Alcohol Abuse
Liver: cirrhosis, alcoholic hepatitis, Liver cancer Malnutrition: Folate and Thiamine CNS effects, Cardiomyopathy, Mild Anemia, Sexual dysfunctioin, respiratory infections (immunosuppressed), Skeletal muscle atrophy, hypothermia, teratogenicity (fetal alcohol syndrome)
202
General Side Effects of Antipsychotics
Decreased seizure threshold, Anticholinergic effects, EPS, Tardive Dyskinesia, NMS.
203
St. John's Wort Drug Interactions
Don't combine with other anti-depressants due to serotonin syndrome.
204
TCA SE
Caused by blocking alpha (cardiac depression, arrhythmias), histamine (drowsiness) and Ach (antichol effects) receptors. Weight gain. Analgesia. SIADH. Sexual dysfunction. Decreased seizure threshold. No euphoria (low abuse potential). Can be used in pregnancy.
205
Bromocriptine
Ergot derivative that acts as a DA D2 agonist. Side effect of erythromelalgia. Can be used to decrease craving for cocaine.
206
Chloral Hydrate
Sedative-Hypnotic. Not highly recommended (low margin of safety) but extremely cheap. Often used in nursing homes.
207
Lamotrigine SE
Dizziness, HA, N/V, SJS, rash, teratogenic.
208
Barbituates Contraindications
Pulmonary insufficiency, Porphyria (increases porphyrin synthesis).
209
Levodopa (L-dopa) MOA
Replacement therapy for Parkinson's. L-dopa can cross the BBB where it is converted into DA (only 1-3% gets into the brain).
210
Barbituates MOA
CNS depressant (hypnosis). GABAa agonist. Binds the receptor and increases the duration of GABA action. Occurs Independent of GABA. No ceiling effect (Low margin of safety).
211
Metaxalone methocarbamol
Acute local muscle relaxant.
212
Zaleplone
Z-Drug. Short duration of action.
213
Benzotropine
Muscarinic receptor antagonist, restores Ach and DA balance. Used as an adjunct to improve rigidity and tremor.
214
TCA Indications
Chronic TMJ pain, Fibromyalgia, Depression (last drug of choice).
215
Articaine
Amide LA that also has an ester group so metabolized via plasma esterases. Used commonly in dentistry.
216
Buproprion MOA
Anti-depressant. Inhibits DA reuptake (little NE and 5HT).
217
Tardive Dyskinesia (TD)
Side effect of antipsychotics (least likely to occur with clozapine and olanzapine) especially after long term treatment. Chreiform, uncontrolled jerky movements.
218
Methanol Poisoning Presentation
Visual disturbances (being in a snow storm), formaldehyde on breath. Severe metabolic acidosis.
219
Wernicke-korsakoff syndrome
paralysis of eye muscles, ataxia, confusion, coma and dearh. Due to thiamine deficiency.
220
Disulfuram (antabuse) Indications
Treatment of alcoholism. Not often used. Dangerous.
221
Mesocortical DA Pathway
VTA to the frontal cortex. Cognition and Emotion. Not enough DA causes the negative symptoms of schizophrenia.
222
Prilocaine
Amide LA. Immediate duration of action. Has the highest rate of clearance of the amides. Risk of methemoglobinemia.
223
Local Anesthetics Transport Across the Membrane
Local Anesthetics are weak bases. Must be nonionized to cross the cell membrane. The closer their Pka is to 7.4 the higher concentration is nonionized so the faster it is transported. Inflammation (more acidic) decreases onset of action and bicarb increases the onset of action.
224
Atypical Antipsychotics MOA
Blocks 5HT2a and DA D2 and D4 receptors. Targets the mesocortical and mesolimbic systems. Alleviates both positive and negative symptoms.
225
Carbidopa MOA
Inhibits dopa-decarboxylase in the periphery. Combined with L-Dopa to decrease the peripheral effects (N/V).
226
Treatment of Anxiety in Children
Anti-Depressants
227
Lithium Drug interactions
NSAIDs: Increase toxicity. Diueretics: Alter clearance. Competes with Na for reabsorption in the kidney. Decreased Na causes increased lithium toxicity. Increased Na causes an increased excretion of lithium. Increased Lithium causes hyponatremia.
228
Phenytoin/Fosphenytoin Metabolism
Metabolized by and induces and inhibits CYP450s. First order elimination at low doses, Zero order elimination at therapeutic doses.
229
Carbidopa SE
Postural hypotension, Arrhythmias, HTN, Dyskinesias
230
Aripiprazole (Abilify) MOA
Atypical Antipsychotic. Partial agonist for DA D2 and 5HT1a. Antagonist for 5HT2a. "DA system stabilizer" acitvate receptors when DA is too low and blocks them if DA is too high.
231
Acute Alcohol Toxicity Treatment
Manage respirations and prevent emesis. Seizures: Lorazepam or phenytoin.
232
Local Anesthetics General MOA
Block Na channels to inhibit neuronal firing. Higher affinity for channels in activated or inactivated state, not in resting state. Block in more effective in rapidly firing axons. Elevated Ca will diminish the block and elevated K will increase the block.
233
Sertraline
SSRI. Preferred in the elderly. Least drug interactions of the SSRIs.
234
Cocaine Addiction treatment
Bromocriptine can decrease craving.
235
Ramelteon SE
Drowsiness, dizziness, nausea. Additive sedation with alcohol.
236
Buprenorphine MOA
Mixed Opiod. Partial Mu agonist with some Kappa. Often mixed with naloxone (inhibits effects if injected).
237
SSRI Indications
Depression, panic disorder, bulimia, alcoholism, and depression in children.
238
Valproic Acid SE
Alopecia, hepatotoxictiy, teratogenic.
239
Alcohol Withdrawal Presentation
Mild anxiety, irritability, insomnia, nausea, tachycardia. Hallucinations, DTs, seizures, hypotension, arrhythmias.
240
Buspirone MOA
Sedative-hypnotic. Partial agonist at postsynaptic 5HT (inhibits signaling) and full agonist at presynaptic 5HT (decreases release of 5HT).
241
Acute Local Muscle Relaxant MOA
Acts at the brain stem to decrease neuronal activity in the spinal cord.
242
Gabapentin Metabolism
First order elimination. Excreted by the kidneys. Negligible drug interactions.
243
MDMA (ecstasy)
Increases 5HT by blocking reuptake and stimulating 5HT receptors. Not addictive because doesn't effect DA. Leads to hyperthermia and dehydration. Can have persistent memory loss.
244
Chlorpromazine SE
High anticholinergic effects so low risk of EPS. Retinal deposits and decreased seizure threshold.
245
Phenytoin/Fosphenytoin Indications
Partial and TC seizures.
246
Tetracaine
Ester LA. 16x more potent that procaine. Ophthalmologic use (retrobulbar).
247
Oxycodone
Moderate Opiod. Activated by CYP2D6 (variable metabolizers.
248
Dibucaine
Dibucaine number test to determine butyrylcholinesterase activity to identify mutations or deficiencies.
249
Marijuana (THC)
Targets presynaptic cannabinoid (CB1) receptors and inhibits neurotransmitter release (Ach and glutamate). No physiologic dependence but psychological dependence is possible. Amotivational syndrome.
250
Naltrexone SE
Liver damage. Don't use in patients with liver failure. Will precipitate with chronic opiod users.
251
Opiod Drug Interactions
Seadtive-hypnotics: CNS and respiratory depression Antipsychotics: sedation and respiratory depression MAOIs: meperidine and dextro can cause serotonin syndrome. Fluoxetine: inhibits metabolsim of coedine to morphine.
252
Cyclobenzaprine
Acute local muscle relaxant. Has antimuscarinic action so causes sedation.
253
Oxazepam
Intermediate-acting Benzodiazepine.
254
Vigabatrin MOA
Anti-convulsant. Irreversibly inhibits AB transaminase (GABA-T) to decrease GABA metabolism.
255
Benzodiazepines SE
CNS depression (tolerance will develop), paradoxical excitement (elderly), Sleep related behaviors. High abuse potential.
256
Halperidol
Classical Antipsychotic. Injected for acute psychosis. No anticholinergic effects so high risk of EPS.
