CNS Flashcards
Fluoxetine mechanism of action
SSRI
Selective blockade of 5HT reuptake
Amitriptyline mechanism of action
TCA
Nonspecific blockade of 5HT and NE reuptake
Phenelzine mechanism of action
Inhibits MAOA and MAOB
Carbamazapine adverse affects
- CNS depression
- Osteomalacia
- Megaloblastic anemia
- Aplastic anemia
- Exfoliative dermatitis
- Increase ADH secretion causing dilutional hyponatremia
Gabapentin mechanism of action and use
- Increase GABA effect
- Used in seizure states, neuopathic pain (postherpetic neuralgia)
Nigrostriatal tract
- Cell bodies in the substantia Nigra project to the stritum where they release DA which inhiits GABA-ergic neurons
- In Parkinsons, loss of DA neurons leads to excessive ACh activity
Amides and esters (local anesthetics) co-adminstered with? And why?
Alpha 1 agonist
- Decreas local anesthetic absorption into the system circulation
- Prolong effect and decrease toxicity
D2 second messenger
Gi
SSRI’s are used for
- Major depression
- OCD
- Bulimia
- Anxiety disorders
- Premenstrual dysphoric disorder (PMDD)
Phenytoin pharmacokinetics
- Variable absorption
- Nonlinear kinetics
- Induction of Cytochrome P450
- Zero-order kinetic of elimination
Lithium teratogenicity
Causes Ebstein’s anomaly (Malformed tricuspid valve)
Withdrawl signs of BZ
- Anxiety
- Rebound insomnia
- Seizure when BZ are used as antiepileptic or in High doses
Meperidine chx:
- Full opiod agonist
- Also antimuscarinic so causes no miosis, tachycardia and no GI/GU/GB spasms
- Metabolized by P450 to normeperidine, a serotonin reuptake inhibitor. May cause serotonin syndrome and seizures
Selegiline mechanism of action
MAOB Selective inhibitor preventing DA breakdown to metabolites
Lithium adverse affects
- Tremor, flu-like symptoms, seizures
- Hypothyroidism with goiter (due to inhibition of 5’-deiodinase)
- Nephrogenic DI (Decrease ADH) [manage with AMILORIDE]
Withdrawl signs of Barbs
- Anxiety
- Agitation
- Life-threatening seizures
Buprenorphine CHX:
- Partial opiod agonist
- Used for precipation of withdrawl
Lithium mechanism of action
- Prevents recycling of Inositol (Decrease in PIP2) by blocking Inositol monophosphatase
- Decrease cAMP
Alcohol in pregnancy causes
- Growth restriction
- Midfacial hypoplasia
- microcephaly
- CNS dysfunction
- frequent occurrence of mental retardation
Methadone CHX:
- Full opiod agonist
- Used in maintenance of opiate addiction
Amides and esters (Local anesthetics) mechanism of action
- Ionized form blocks internal inactivated Na channel in axon
Clozapine CHX:
Atypical antipsycotic
Blocks D2c and 5HT2 receptors
NO TD
Benzodiazepine mechanism of action
Potentiates GABA causing increased frequency of Cl channel opening
Alprazolam indication
BZ
- Anxiety
- Panic
- Phobias
Barbiturate mechanism of action
Prolong GABA activity by increaing duration of Cl channel opening
Also inhibits Complex 1 of ETC
TCA toxicity
3 C’s
- Coma
- Convulsions
- Cardiotoxicity
Nalbuphine CHX:
- Mixed opiod agonist - antagnoist
- Kapa Agonist: Spinal analgesia and dysphoria
- Mu antagonist: Precipitation of withdrawl
D2A found in
Nicrostriatal
Mirtazapine CHX:
Antidepressant that is an ALPHA 2 antagonist associated with weight gain
SSRI adver affects
- Anxiety
- Agitation
- Bruxism
- Sexual dysfuntion
- Weight loss
Olanzapine EPS, M Block, Sedation and Alpha Block:
Atypical Antipsycotic
EPS: -/+
M Block: +
Sedatoin: +
Alpha Block: ++
Risperidone EPS, M Block, Sedation and Alpha Block:
Atypical Antipsycotic
EPS: +
M Block: +/-
Sedation: ++
Alpha Block: ++
Acute adverse affects of opiods
- Pinpoint pupils
- Respiratory depression
- Coma
When to caution with Morphine
- Head trauma due to vasodilation
- Renal dysfuntion due to morphine metabolite is active
Disulfiram-like drugs
- Metronidazole
- Chlorpropamide
- Griseofulvin
Carbamazepine mechanism of action
Blocks axonal Na channels in their inactivated state decreasing axonal conduction preventing seizure propagation
Phenelzine and Tranylcypromine used for
MOA inhibitors used for atypical depression
Pharmocologic goal in Parkinsons
Increase DA and decrease ACh
Buspirone mechanism of action
5-HT1A Partial agonist that has no effect on GABA therefore it is NON sedative but takes 1 to 2 wks for effect
Nondepolarizing skeletal mucle blockers Mechanism and CHX
- Nicotinic antagonists
- Reversible with AChEI
- No effects on cardiac and smooth muscle
- No CNS effects
Diazepam indicaiton
BZ
- Anxiety
- Peop sedation
- Muscle relaxation
- Withdrawal state
Oxazepam indication
BZ
- Sleep disorder
- Anxiety
Tolcapone Mechanism of action
Inhibits COMT from converting L-Dopa to 3-O-methyldopa (a partial agonist at DA receptor)
Felbamate is
Same as lamotrigine by blocking Na channels and glutamate receptors
In partial seizures (simple or complex) give
- Valproic acid
- Phenytoin
- Carbamazepine
- Lamotrigine
Aripiprazole CHX:
Atypical Antipsycotic
Partial agonist of D2 receptors
Blocks 5HT2 receptors
Lamotrigine adverse affects
Steven-Johnson syndrome (skin rash)
Levodopa adverse affects
- Dyskinesias
- “on-off” effect
- Psychosis
- Hypotension
- Vomiting
Antipsycotics adverse affects from DA block
- Dyskinesias (extrapyramidal symptoms)
- Dysphoria
- Endocrine dysfunction: Tem regulation problems, Increase Prolactin, Increase eating
Ethosuximide mechanism of action
Blocks T-type Ca channels in thalamic neurons
Lorazepam indication
BZ
- Anxiety
- Preop sedation
- Status epilepticus (IV)
Ketamine adverse affects
- Cardiovascular stimulation
- Increase intracranial pressure
Zolpidem and Zaleplon overdose reversed by
Flumazenil
Valproic acid adverse affects
- Hepatotoxicity from metabolites
- Thrombocytopenia
- Pancreatitis
- Alopecia
Phenytoin adverse affects
- CNS depression
- Gingival hyperplasia
- Hirsutism
- Osteomalacia (decreas Vit D)
- Megaloblastic anemia (decrease Folate)
- Aplastic Anemia (check hematology)