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113 Cards in this Set
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Chlorpromazine (Thorazine)
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Antipsychotics
Affect dopaminergic pathway Regulation of motor control, mood, & emotion Inhibitory on neuron onto which it is released Aside: Loss of dopaminergic neurons- symptoms commonly assoc. w/ Parkinson's & Schizophrenia Receptor Subtype & Effect: D1 & D2- Inhibitory (D3-5 not specified) **DOPAMINE |
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Amphetamine (Adderall)
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*Considered inhibitory but can be excitatory
CNS Stimulant Affect dopaminergic pathway Regulation of motor control, mood, & emotion Inhibitory on neuron onto which it is released Aside: Loss of dopaminergic neurons- symptoms commonly assoc. w/ Parkinson's & Schizophrenia Receptor Subtype & Effect: D1 & D2- Inhibitory (D3-5 not specified) --------------------------------------------- NE- affect noradrenergic pathways Inhibitory NT - Alpha 2 Excitatory NT - Alpha 1 or Beta A1- Excitatory A2- Inhibitory B1- Excitatory B2- Inhibitory **DOPAMINE & NE |
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Levodopa (Larodopa)
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Antiparkinson's Agent
Affect dopaminergic pathway Regulation of motor control, mood, & emotion Inhibitory on neuron onto which it is released Aside: Loss of dopaminergic neurons- symptoms commonly assoc. w/ Parkinson's & Schizophrenia Receptor Subtype & Effect: D1 & D2- Inhibitory (D3-5 not specified) **DOPAMINE |
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Selegiline (Emsam)
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*Considered inhibitory but can be excitatory
Monoamine Oxidase Inhibitor NE- affect noradrenergic pathways Inhibitory NT - Alpha 2 Excitatory NT - Alpha 1 or Beta A1- Excitatory A2- Inhibitory B1- Excitatory B2- Inhibitory **NE |
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Amitriptyline (Elavil)
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*Considered inhibitory but can be excitatory
Tricyclic Antidepressant NE- affect noradrenergic pathways Inhibitory NT - Alpha 2 Excitatory NT - Alpha 1 or Beta A1- Excitatory A2- Inhibitory B1- Excitatory B2- Inhibitory **NE |
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Donepezil (Aricept)
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Acetylcholinesterase Inhibitor
Affects the activity of of cholinergic system Excitatory transmitter in CNS Inhibitory transmitter in PNS Cognition & Memory- Alzheimer's *ACh |
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Benztropine (Cogentin)
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Muscular Blocking Agent
Affects the activity of of cholinergic system Excitatory transmitter in CNS Inhibitory transmitter in PNS Cognition & Memory- Parkinson's **ACh |
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Serotonin
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Tricyclic Antidepressants & SSRI's
Primarily Strong Inhibitory NT Control mood & behavior (depression & anxiety) 5HT1a- Inhibitory 5-HT-2a- Excitatory 5-HT-3- Excitatory 5-HT-4- Excitatory |
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Memantine (Namenda)
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Major excitatory NT found in Cerebral Cortex & Brain Stem (NMDA Receptors)
Plays a role in memory & learning Alzheimer's 4 NMDA Subtypes- Excitatory Metabolic Subtypes- Inhibitory **GLUTAMATE (ASPARTATE) Glutamate may also produce neurotoxic effects when released in large amounts during CNS injury & certain neurologic disorders leading to cell death (Ex. Epilepsy & ALS) |
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Benzodiazepines, barbiturates
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GABA-A
Sedative hypnotics GABA: -Important inhibitory transmitter at pre- & post- synaptic neurons in brain & SC -Many sedate/tranquilizing drugs act by enhancing the effects of GABA GABA-A: Inhibitory GABA-B: Inhibitory |
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Gabapentin (Neurontin)
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GABA-A
Anticonvulsant GABA: -Important inhibitory transmitter at pre- & post- synaptic neurons in brain & SC -Many sedate/tranquilizing drugs act by enhancing the effects of GABA GABA-A: Inhibitory GABA-B: Inhibitory |
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Baclofen (Kemstro)
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GABA-B
Muscle Spasticity GABA: -Important inhibitory transmitter at pre- & post- synaptic neurons in brain & SC -Many sedate/tranquilizing drugs act by enhancing the effects of GABA GABA-A: Inhibitory GABA-B: Inhibitory |
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Peptide Transmitters
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Opioid Peptides- Morphine
Substance P- Excitatory transmitter involved in SC pathways transmitting pain impulses -Certain drugs such as the opiod analgesics may Decrease activity at these synapses Endorphins, Enkephalins, & dynorphin Family- ENDOGENOUS OPIODS; • EXCITATORY transmitters in certain BRAIN SYNAPSES that INHIBIT PAINFUL SENSATION; Able to Decrease CENTRAL PERCEPTION OF PAIN Receptor Subtypes: Mu Delta Kappa **Inhibitory |
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Benzodiazepines
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Sedative - Hypnotic
Therapeutic Uses: 1. Anxiety disorders 2. Panic disorders 3. Skeletal muscle spasm 4. Status Epilepticus 5. EtOH withdrawal (Chlordiazepoxide) 6. Insomnia -Dose Dependent -Relieve anxiety --> Induce sleep --> Anesthetic Effects BZD binds GABA-A receptor complex (Bound to Cl- Channel) which enhances GABA effects or inhibits NT --> Increased frequency of channel opening --> Increase Cl- flux into cell --> Hyperpolarization --> Inhibition of cell activity/decreased neuronal firing --> Effects: Sedative, Hypnotic, Anticonvulsant, Muscle-Relaxant -Highly Lipid Soluble: Crosses BBB- FAST Onset of action -HEPATIC Oxidation: Long ½ life; active metabolites -Glucurronidation: SHORT ½ life; NO active metabolites Cross placental barrier & enter breast milk Adverse Effects: 1. Sedation, CNS Depression (Worse if combined w/ EtOH) 2. Behavioral DIS-INHIBITION (Irritability, excitement, aggression (<1%), rage) 3. Psychomotor & Cognitive Impairment (Coordination, attention (driving), memory impairment; Poor visual-spatial ability (Not Aware of It); Confusion) 4. OD Can be fatal 5. Severe CNS & Respiratory Depression if combined with: o ETOH o Barbiturates o Narcotics o Tricyclic antidepressants |
Dependence & withdrawals
1. Alprazolam & Triazolam LOW street value due to sedation 2. Increase lipophilic 3. Increased abuse potential 4. Short ½ life 5. More intense withdrawals Withdrawals 1. Worse if stopped abruptly 2. Symptoms- GI, excessive sweating, Increased pulse, Increased BP 3. Tremors, Lethargy, Dizziness, HA 4. Restlessness, insomnia, irritability, anxiety 5. Depersonalization, perceptual disturbances Depression, ringing in the ears, delirium, panic, hallucinations, abnormal muscular movs. Seizures: abrupt discontinuation of short acting |
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Oxazepam (SERAX)
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Sedative - Hypnotic
Short acting (3-8 hours) Benzodiazepines (BZD) |
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Midazolam (VERSED)
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Sedative - Hypnotic
Short acting (3-8 hours) Benzodiazepines (BZD) |
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Triazolam (HALCION)
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Sedative - Hypnotic
Short acting (3-8 hours) Benzodiazepines (BZD) |
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Alprazolam (XANAX)
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Sedative - Hypnotic
Intermediate (10-20 hrs) Benzodiazepines (BZD) |
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Lorazepam (ATIVAN)
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Sedative - Hypnotic
Intermediate (10-20 hrs) Benzodiazepines (BZD) |
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Temazepam (RESTORIL)
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Sedative - Hypnotic
Intermediate (10-20 hrs) Benzodiazepines (BZD) |
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Estazolam (PROSOM)
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Sedative - Hypnotic
Intermediate (10-20 hrs) Benzodiazepines (BZD) |
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Chlodiazepoxide (LIBRIUM)
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Long (1-3 days)
Benzodiazepines (BZD) Therapeutic Use: EtOH Withdrawal |
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Diazepam (VALIUM)
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Sedative - Hypnotic
Long (1-3 days) Benzodiazepines (BZD) |
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Halazepam (PAXIPAM)
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Sedative - Hypnotic
Long (1-3 days) Benzodiazepines (BZD) |
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Flurazepam (DALMANE)
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Sedative - Hypnotic
Long (1-3 days) Benzodiazepines (BZD) |
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Quazepam (DORAL)
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Sedative - Hypnotic
Long (1-3 days) Benzodiazepines (BZD) |
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Oxazepam (SERAX)
Midazolam (VERSED) Triazolam (HALCION) |
Sedative - Hypnotic
Short (3-8 hours) Benzodiazepines (BZD) |
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Alprazolam (XANAX)
Lorazepam (ATIVAN) Temazepam (RESTORIL) Estazolam (PROSOM) |
Sedative - Hypnotic
Intermediate (10-20 hrs) Benzodiazepines (BZD) |
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Chlodiazepoxide (LIBRIUM)
Diazepam (VALIUM) Halazepam (PAXIPAM) Flurazepam (DALMANE) Quazepam (DORAL) |
Sedative - Hypnotic
Long (1-3 Days) Benzodiazepines (BZD) |
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Clonazepam (KLONOPIN)
Clorazepate (TRANXENE) |
Sedative - Hypnotic
Benzodiazepines (BZD) |
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FLUMAZENIL (ROMAZICON)
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Sedative - Hypnotic
BZD ANTAGONIST / Blocks action of BZDs Reverse BZD OD & to speed up recovery following use of BZDs in anesthetic or diagnostic procedure IV admin. |
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Barbiturates
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Sedative - Hypnotic
Facilitate actions of GABA Increase the DURATION of Cl- channel opening (unlike BZD which Increase frequency NOT USED FOR ANXIETY OR INSOMNIA Potentially FATAL Respiratory Depression Narrow therapeutic range Potent liver inducers: interactions |
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Amobarbital (AMYTAL)
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Sedative - Hypnotic
Sedative Barbiturates |
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Pentobarbital (Nembutal)
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Sedative - Hypnotic
Sedative Barbiturates |
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Phenobarbital (Luminal Sodium)
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Sedative - Hypnotic
Anticonvulsant Barbiturates |
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Secobarbital (Seconal)
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Sedative - Hypnotic
Barbiturate Does not respond to BZD antagonist Flumazenil (OD, etc.) |
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Thiopental (Pentothal)
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Sedative - Hypnotic
ULTRA SHORT ½ life IV Gen. Anesthesia Barbiturates |
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Antihistamines
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Sedative - Hypnotic
Non-BZD Hypnotic agent |
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Chloral Hydrate
(Somnote, noctec) |
Sedative-Hypnotic
Non-BZD |
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Eszopiclone
(Lunesta) |
Sedative-Hypnotic
Non-BZD Binds selectively to ONLY GABA-A receptors forms the contain ALPHA-1 subunits Stim. of this particular subunit seems to mediate sedation w/o producing other side effects |
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Ethanol
(alcohol, grain alcohol) Various |
Sedative-Hypnotic
Non-BZD |
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Ramelteon
(Rozerem) |
Sedative-Hypnotic
Non-BZD |
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Zaleplon
(Sonata) |
Sedative-Hypnotic
Non-BZD Binds selectively to ONLY GABA-A receptors forms the contain ALPHA-1 subunits Stim. of this particular subunit seems to mediate sedation w/o producing other side effects |
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Zolpidem
(Ambien) |
Sedative-Hypnotic
Non-BZD Binds selectively to ONLY GABA-A receptors forms the contain ALPHA-1 subunits Stim. of this particular subunit seems to mediate sedation w/o producing other side effects |
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Buspirone
(Buspar) |
Sedative-Hypnotic
Non-BZD Agonist at 5-HT-1a receptors Non-sedating, NO PHYSICAL DEPENDENCE or withdrawal; No interaction w/ ETOH Slow onset of action (2-4 hours) Adverse effects: Increased HR; HA; Dizziness; Nervousness Therapeutic Use: Anxiety & Depression |
Good for elderly pts or pts w/ substance abuse problems
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Eszopiclone (Lunesta)
Zolpidem (Ambien) Zaleplon (Sonata) |
Sedative-Hypnotic
Non-BZD Binds selectively to ONLY GABA-A receptors forms the contain ALPHA-1 subunits Stim. of this particular subunit seems to mediate sedation w/o producing other side effects |
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Hydroxyzine (Atarax)
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Sedative-Hypnotic
Non-BZD Therapeutic Use: Anxiety & insomnia Some anticholinergic effects Non-addicting |
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Primary Epilepsy
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Specific causative factor cannot be found
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Secondary or Symptomatic Epilepsy
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Brought on by:
1. Tumor 2. Head Trauma 3. Stroke 4. Congenital abnormality/Genetic factor 5. Underlying acute toxic or metabolic disorder (Infection, Hypoglycemia, Poisoning) |
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Partial Seizures
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Focal Onset
Affect only a PART of the brain at ONSET Consciousness is usually PRESERVED May progress to become generalized tonic-clonic seizures |
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Simple Partial Seizures
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Consciousness is NORMAL
Abnormal electrical activity confined to a single place in the brain Electrical discharge does not spread & pt does not lose consciousness Pt often exhibits abnormal activity of a single limb or muscle group that is controlled by the region of the brain experiencing the disturbance Simple & partial seizure activity may spread to become complex the spread to a secondary generalized convulsion |
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Complex Partial Seizures
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Larger Seizure
Impairment of consciousness/no memory -Affects a larger part of the brain hemisphere than a simple seizure Either simple or complex partial seizures may become secondarily generalized, producing a tonic-clonic seizure -If it spreads from 1 hemisphere → other side of brain Exhibit complex sensory hallucinations & mental disorientation Motor dysfunct. May involve chewing movements, diarrhea, &/or urination Consciousness is altered |
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Generalized Seizures
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Bilateral Onset
Impairs consciousness & distorts the electrical activity of the whole or larger portion of the brain May be convulsive or non-convulsive Usually has an IMMEDIATE LOC |
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Tonic-Clonic
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Generalized Seizures (Bilateral Onset)
Formerly: Grand Mal Results in LOC; followed by tonic (continuous contraction) & clonic (rapid contraction & relaxation) phase Seizure may be followed by a period of confusion & exhaustion due to the depletion of glucose & energy stores |
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Absence
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Generalized Seizures (Bilateral Onset)
Brief, abrupt, & self-limiting LOC (<30 sec) Pt stares & exhibits RAPID-EYE BLINKING, (3-5 sec.) |
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Myoclonic
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Generalized Seizures (Bilateral Onset)
Extremely brief episodes of muscle contraction that may recur for several minutes Generally occur after wakening & exhibit brief jerks of limb |
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Status Epilepticus
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Generalized Seizures (Bilateral Onset)
2+ seizures (usu. Tonic-clonic) occur w/o recovery of full consciousness btwn them LIFE-THREATENING & requires emergency treatment (brain damage) |
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Carbamazepine
Phenytoin Lamotrigine Valproic Acid |
Used to treat Tonic-Clonic & Partial Seizures
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Ethosuximide
Valproic Acid Clonazepam Lamotrigine |
Used to treat Absence Seizures
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Valproic Acid
Clonazepam |
Used to treat Myoclonic Seizures
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Felabmate
Gabapentin Lamotrigine Levetiracetam Phenobarbital Tigabine Topiramate Vigabatrin Zonisamide |
Back-Up & Add-on Therapy for Seizures
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Phenytoin (Dilantin)
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MOA:
-Block Na+ channels -Inhibit the generation of repetitive action potentials → Suppress epileptic focus -Block Ca2+ Influx → INHIBITION of seizure spread Uses: -Initial drug of choice in all types of epilepsy EXCEPT FOR ABSENCE SEIZURES -Most efficacious against: 1. Partial Seizures 2. General Tonic-Clonic Seizures Adverse Effects: -From chronic administration 1. Gingival Hyperplasia (20%) - Common in children 2. Hirsutism -Neurotoxicity is dose related 1. Nystagmus 2. Ataxia 3. Slurred speech 4. Drowsiness - Fetal abnormalities **- Stevens-Johnson Syndrome- Severe skin condition (can be fatal) Blistering & Erosion of the skin & mucous membranes **MUST DC MED IS THIS OCCURS |
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Fosphenytoin (Cerebryx)
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More soluble than phenytoin
Used EXCLUSIVELY in PARENTERAL RX STATUS EPILEPTICUS Side Effect profile comparable to phenytoin -From chronic administration 1. Gingival Hyperplasia (20%) - Common in children 2. Hirsutism -Neurotoxicity is dose related 1. Nystagmus 2. Ataxia 3. Slurred speech 4. Drowsiness - Fetal abnormalities **- Stevens-Johnson Syndrome |
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Carbamazepine (Tegretol)
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MOA: Blockage of Na+ Channels & inhibits high-frequency repetitive firing in neurons → stabilizing membranes
Drug of choice for: 1. Partial Seizures 2. Gen. Tonic-Clonic Seizures Advantage 1. NOT Sedative in Therapeutic Range Side Effects 1. GI Upset 2. CNS: Vertigo, diplopia, blurred vision, ataxia 3. Stevens-Johnson Syndrome 4. Hematological Disorder: (Aplastic Anemia, Thrombocytopenia, Agranulocytosis, Leukopenia) 5. Liver Toxicity – MUST MONITOR |
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Phenobarbital (Luminal)
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MOA: Selectively suppresses abnormal neurons; Enhances GABA-mediated chloride flux that causes membrane HYPERpolarization → may block the excitatory NT Glutamate
Uses 1. Partial seizures & generalized tonic-clonic seizures 2. Can be used for ALL other types of seizures when they are difficult to control 3. Drug of choice for infants with seizures ** Adverse Effects 1. Sedation |
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Diazepam (Valium)
Lorazepam (Ativan) |
BZDs
Enhance inhibitory effects of GABA Uses: Acute IV treatment of STATUS EPILEPTICUS Adverse Effects 1. Sedation 2. Tolerance 3. Dependence Caution: Abrupt withdrawal causing seizures |
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Clorazepate (Tranzene)
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BZD
Enhance inhibitory effects of GABA Add on in COMPLEX PARTIALSEIZURES Adverse Effects 1. Sedation 2. Tolerance 3. Dependence Caution: Abrupt withdrawal causing seizures |
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Clonazepam (Klonopin)
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BZD
Enhance inhibitory effects of GABA Uses: ABSENCE SEIZURES & MYOCLONIC SEIZURES Adverse Effects 1. Sedation 2. Tolerance 3. Dependence Caution: Abrupt withdrawal causing seizures |
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Gabapentin (Neurontin)
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MOA: Increases release of GABA
Uses 1. Add on for PARITAL SEIZURES & GENERAL TONIC CLONIC SEIZURES 2. Neuropathic pain Adverse Effects 1. Sedation 2. Dizziness 3. Behavioral Changes 4. Weight gain 5. HA 6. Tremor *100% renal elimination |
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Lamotrigine (Lamictal)
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MOA: Inhibition of Na+ Channels → Suppressing rapidly firing neurons
Uses 1. Partial Seizures 2. Absence Seizures 3. Myoclonic Seizures Adverse Effects 1. Sedation 2. Ataxia 3. Nausea 4. Dizziness 5. HA 6. **Steven-Johnson Syndrome |
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Fembamate (Felbatol)
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MOA: Increase GABA & Decrease Glutamate
Uses: 1. Limited due to adverse effects 2. Add on tx PARTIAL SEIZURES or MYOCLONIC SEIZURES Adverse Effects 1. Aplastic Anemia 2. Severe Hepatotoxicity (Very common) Aplastic anemia & hepatic failure Broad spectrum of antiseizure activity Requires pt to sign informed consent at dispensing |
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Tiagabine (Gabitril)
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MOA: Inhibitor of GABA uptake, prolonging the inhibitory effects of GABA
Uses: Add on Tx for PARTIAL SEIZURES Adverse Effects 1. Nervousness 2. Dizziness 3. Tremor 4. Difficulty concentrating 5. Depression 6. Excessive Confusion Multiple drug interactions |
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Topiramate (Topamax)
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MOA: Blockage of voltage dependent Na+ Channels; Increase effects of GABA; Blocks excitatory AA receptors
Uses 1. PARTIAL & GENERALIZED TONIC CLONIC SEIZURES Adverse Effects 1. Sedation 2. Mental dulling 3. Renal stones 4. Wt loss 5. **Stevens Johnson Syndrome Few drug interactions Broad spectrum of antiseizure activity |
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Ethosuximide (Zarontin)
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MOA: Block T-Type Ca2+ channels → Increase in seizure threshold & limit spread of electrical activity in brain
Uses: ABSENCE SEIZURES Adverse Effects 1. GI Irritation: N/V; anorexia 2. CNS Depression: Drowsiness, lethargy, dizziness, HA 3. Rashes: Urticaria, **Stevens-Johnson Syndrome Blood dyscrasias can occur; periodic CBCs should be done Abrupt DC can cause seizures |
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Valproic Acid (Depakote)
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MOA: Increase levels of GABA by inhibition of degradation; Blocks Na+ Channels; Inhibits T-type Ca2+ channels
Uses 1. Absence Seizures 2. Partial seizures 3. General tonic-clonic seizures 4. Myoclonic seizures Adverse Effects 1. Weight gain 2. GI Distress (N/V) 3. Hepatotoxicity 4. Temporary Hair Loss (Hair Thinning) Drug Interactions 1. Causes increase in serum phenytoin levels |
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Stages of GENERAL Anesthesia
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Stage 1: Analgesia
-Pt has decreased awareness of pain, sometimes w/ amnesia -Consciousness may be impaired, but NOT lost Stage 2: Disinhibition/Delirium -Pt is delirious & excited -Amnesia occurs -Reflexes are enhanced -Respiration is irregular -Vomiting & incontinence may occur -Goal= move out of this stage rapidly Stage 3: Surgical Anesthesia -Unconscious & NO pain reflexes -Respiration is regular -BP maintained Stage 4: Medullary Depression -Too deep, essentially produces an OD -Develops severe respiratory & CV depression → requires mechanical & pharm support -W/o support → Death rapidly occurs |
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Nitrous Oxide
Halothane Enflurane Isoflurane Desflurane Sevoflurane Methoxyflurane |
General Anesthetic
Gas form MOA: FACILITATE GABA-mediated INHIBITION at BAGA-A receptors -Ketamine blocks the excitatory NT Glutamate at NMDA receptor Most inhaled anesthetics ALSO INHIBIT nicotinic ACh receptor isoforms at moderate – high concentrations Clinical Use of Inhaled Anesthetics -Usu. Combined with IV agents -Rarely used as the sole agents for induction & maintenance of anesthesia Adverse Effects -CNS: Increases Cerebral blood flow (intracranial pressure) -CV: mod. Decreased BP -Decrease in blood flow to Kidneys & Liver -Ventricular arrhythmias (halothane) -Other 1. Post-op hepatitis (halothane) 2. Muscle spasm |
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Thiopental (Pentothal)
Methohexital (Brevital) Midazolam (Versed) Diazepam (Valium) Morphine Fentanyl (Sublimaze) Sufentanil (Sufenta) Alfentanil (Alfenta) Remifentanyl (Ultiva) Propofol (Diprivan) Ketamine (Ketalar) Droperidol (Inapsine) Etomidate (Amidate) Dexmetomidate (Precedex) |
IV Administered General Anesthetics
IV -Faster onset of action than most of the inhaled gases -Recovery is rapid -Used in many outpt procedures Barbiturates -*Highly lipid soluble → rapid entry into the brain → anesthesia occurs <1’ Uses : -Anesthesia for short surgical procedures Hepatic metabolism required for elimination |
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Midazolam (Versed)
Diazepam (Valium) |
IV Administered General Anesthetics
BZD |
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Midazolam (Versed)
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IV Administered General Anesthetics
BZD Often used w/ inhaled anesthetics & IV opiods Onset is slower then thiopental Longer duration of action |
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Morphine
Fentanyl (Sublimaze) |
IV Administered General Anesthetics
Opioid Analgesic Used with BZDs & NO in anesthesia regimens Especially for high risk pts who will not survive full analgesia Adverse Effects 1. Respiratory depression |
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Morphine
Fentanyl (Sublimaze) Sufentanil (Sufenta) Alfentanil (Alfenta) Remifentanyl (Ultiva) |
IV Administered General Anesthetics
Opioid Analgesic |
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Propofol (Diprivan)
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IV Administered General Anesthetics
Most commonly used IV anesthetic Onset is as rapid as barbiturates (<30”) Duration of action >5’ Recovery is even more rapid Less N/V w/ this drug Uses 1. Induction & maintenance of anesthesia Adverse Effects 1. Marked hypotension (Decreased Peripheral resistance/vasodilation) |
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Ketamine (Ketalar)
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IV Administered General Anesthetics
Produces a state of “dissociative anesthesia” -Pt remains unconscious but has marked analgesia & amnesia CV stimulant -Same chemical class of PCP Adverse Effects 1. Disorientation, hallucinations 2. Increase Cranial pressure 3. Decrease respiratory rate |
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Etomidate (Amidate)
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IV Administered General Anesthetics
Rapid induction Short duration of action Primary advantage is an anesthesia for pt w/ limited cardiac or respiratory reserve Adverse Effects 1. Local pain 2. N/V 3. Prolonged admin: adrenal suppression |
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Propofol (Diprivan)
Ketamine (Ketalar) Droperidol (Inapsine) Etomidate (Amidate) Dexmetomidate (Precedex) |
IV Administered General Anesthetics
"Other" |
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Tetracaine
Procaine Benzocaine Cocaine Bupivacaine Ropivacaine Lidocaine |
LOCAL Anesthetics
Uses 1. Minor skin injuries 2. Various surgical procedures & spinal anesthesia (epidural) 3. Abolish sensation & in higher concentrations motor activity in a limited area fo the body APPLIED or INJECTED to block nerve conduction of sensory impulses from the periphery to the CNS Site & MOA -2 chemical groups 1. Esters 2. Amides -Slow or block depolarization by decreasing Na+ permeability into the nerve cytoplasm, thus inhibiting the flow of K+ out of the cell -Nerve impulse travels from node to node -Effectively block nerve impulse travel Delivery Techniques 1. Topical administration 2. Peripheral nerve blocks 3. Neuraxial (spinal, epidural, or caudal) blocks Adverse Reactions 1. CNS: (Lightheadedness, Sedation, Restlessness, Confusion, Agitation, Convulsion) 2. Respiratory Depression 3. CV: (Myocardial depression & cardiac arrest w/ peripheral vasodilation (exception is cocaine)) 4. Local effects include physical injury caused by poor injection technique 5. Incidence of allergic reactions to amide locals is VERY LOW -*Esthers have a higher rate of allergic reactions than amides |
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Tetracaine
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Local Anesthetic
Long Acting Ester |
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Procaine
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Local Anesthetic
Short Acting Ester |
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Benzocaine
Cocaine |
Local Anesthetic
Surface Acting Ester |
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Bupivacaine
Ropivacaine |
Local Anesthetic
Long Acting Amide |
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Lidocaine
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Local Anesthetic
Medium Acting Amide |
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Levodopa
Carbidopa (Sinemet) |
Parkinson's
Dopaminergic Increase dopamine synthesis of dopamine |
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Levodopa
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Parkinson's
Dopaminergic -Dopamine precursor -Converted to dopamine after crossing the BBB |
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Carbidopa (Sinemet)
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Parkinson's
Dopaminergic -Given to prevent premature conversion of dopamine in the periphery (instead of the brain) iv) *Combination decreases the requirements of levodopa by 75% & results in fewer adverse effects -Effectively ameliorates the signs of Parkinson’s -Tremor, rigidity, & especially BRADYKINESIA Best effects seen in first few yrs of treatment Responsiveness to treatment decrease w/ time (thought to be due to progression of dx) Adverse Effects (most are dose dependent) 1. Anorexia, N/V (from stimulation of emetic center) -Tolerance developes, can take in divided doses or w/ food to help 2. Arrhythmias (from dopaminergic action on the ehart) -Especially in pts w/ heart disease 3. Orthostatic Hypotension (especially in early tx) 4. Involuntary movements (dyskinesia) 5. Psychosis (20%)- hallucinations, vivid dreams, paranoid feelings -Decreased dosage, can give 6. Mood changes, depression, anxiety 7. Contraindicated in pts w/ a hx of psychosis |
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Bromocriptine (Parlodel)
Pergolide (Permax) Pramipexole (Mirapex) Ropinirole (Requip) |
Dopamine Agonist
Stimulates dopamine receptors directly Actions similar to levodopa but.. 1. No dependence on enzymatic conversation 2. No conversion to toxic metabolites 3. Decreased incidence response failure First choice for mild – moderate symptoms of Parkinson’s (NEWER AGENTS) Can be sed as monotherapy or in combination w/ levodopa or anticholinergic drugs |
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Bromocriptine (Parlodel)
Pergolide (Permax) |
Dopamine Agonist
Older Agents Dose built up slower over 2-3 months to the desired therapeutic level |
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Pramipexole (Mirapex)
Ropinirole (Requip) |
Dopamine Agonist
Newer Agents Dose built up over 3-4 weeks Less Side effects than older Similar Adverse effects to levodopa EXCEPT: 1. Hallucinations, Confusion, Delirium, Nausea, Orthostatic Hypotension – MORE COMMON 2. Dyskinesia is LESS COMMON than levodopa |
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Selegiline (Eldepryl)
Rasagiline (Azilect) |
MOA B Inhibitor (Monoamine Oxidase Inhibitor)
Prevents dopamine breakdown Selectively inhibits MOA Type B 1. MOA B is an enzyme that metabolizes dopamine (into NE & Serotonin) 2. Enables dopamine to be active for longer periods 3. At higher doses the selectivity is LOST -It will inhibit MOA-A producing antidepressant effects Used as an adjunct to levodopa 2nd & 3rd line Can reduce “wearing off” effect with levodopa Many adverse effects 1. Insomnia (most common)- Can be minimized by taking early in the day 2. Mood changes, dyskinesias, GI distress, & HTN |
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Selegiline (Eldepryl)
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MOA B Inhibitor (Monoamine Oxidase Inhibitor)
Produces active metabolites & small quantities of amphetamine & methamphetamine |
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Rasagiline (Azilect)
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MOA B Inhibitor (Monoamine Oxidase Inhibitor)
Does not form metabolites Reported to have FEWER side effects than Selegline |
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Entacapone (Comtan)
Tolcapone (Tasmar) |
Parkinson's
COMT Inhibitors (Catechol-O-Methyltransferase) Block degeneration of dopamine by inhibiting COMT enzyme peripherally Selective inhibitors of COMT 1. COMT is an enzyme that converts levodopa to 3OMD (inactive metabolite that competes w/ levodopa to the CNS) Prolong the action of levodopa by: 1. Increase the amount transported with the BRAIN 2. Diminishing its PERIPHERAL concentration Helpful in pts on levodopa who have developed response fluctuations 1. Improves response & prolonging “on” time Also provides the opinion of decrease the total daily levodopa dose Adverse Effects 1. Related to increased levels of levodopa -Dyskinesias, Hypotension, Confusion, GI distress |
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Entacapone (Comtan)
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Parkinson's
COMT Inhibitors (Catechol-O-Methyltransferase) Adverse Effect: NO Hepatotoxicity AE: Usually preferred over Tasmar |
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Tolcapone (Tasmar)
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Parkinson's
COMT Inhibitors (Catechol-O-Methyltransferase) Adverse Effect: Assoc. w/ Hepatotoxicity (LFT Monitoring) |
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Amantadine (Symmetrel)
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Parkinson's
Antiviral agent that promotes dopamine synthesis & blocks reuptake -Inhibits the NMDA receptor causing a decrease in the stimulation of ACh Improves bradykinesia, rigidity, & tremor -For only limited time (weeks) Less potent than levodopa Promotes dopamine release Block reuptake Adverse Effects -Many CNS side effects: 1. Restlessness 2. Agitation 3. Insomnia 4. Confusion 5. Acute Toxic Psychosis 6. Reversible once drug is DC -Peripheral Edema 1. Responds to diuretics |
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Benztropine (Cogentin)
Orphendrine (Norflex) Procycline (Kemmadrin) Trihexyphenidyl (Artane) |
Parkinson's
Anticholinergic / ACh Blocking Drugs (Antimuscarinic) Block muscarinic receptor in striatum Decrease the excitatory actions of cholinergic neurons on cells in the striatum by blocking muscarinic receptors Improve tremor & rigidity (50%) Have LITTLE effect on bradykinesia Have value in decreased extrapyramidal symptoms (EPS) effects of atypical antipsychotics (haloperidol) -EPS are drug induced movement disorders Adverse Effects 1. CNS (Drowsiness, Inattention, Confusion, Delusions, Hallucinations) 2. Peripheral: ANTI SLUD (Blurred vision, Constipation, Dry mouth, Urinary retention) |
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Reserpine (Serpasil)
Tetrabenazine (Xenazine) Haloperidol (Haldol) |
Huntington's Syndrome
Dopamine depleting drugs |
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Haloperidol (Haldol)
Pimozide (Orap) Carbemazepine (Tegretol) Clonazepam (Klonopin) Clonidine |
Tourette's Syndrome
Chronic multiple involuntary tics (blinking, turning head, smacking lips) involving sudden violent movements & load vocalizations |
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Haloperidol (Haldol)
Pimozide (Orap) |
Tourette's Syndrome
Dopamine receptor blockers |
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Carbemazepine (Tegretol)
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Tourette's Syndrome
Na+ channel blocker |
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Clonazepam (Klonopin)
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Tourette's Syndrome
BZD |
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Clonidine
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Tourette's Syndrome
Alpha-2 Agonist |
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Penicillamine (Cuprimine)
Trientine (Syprine) |
Wilson’s Disease
Inherited disorder of copper metabolism Copper deposits in the liver & other tissues including the brain Pts exhibit hepatic & neurologic dysfunction |
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