Pharm list for Neuro Exam 4 Flashcards Preview

Pharm list for Neuro Exam 4 > Pharm list for Neuro Exam 4 > Flashcards

Flashcards in Pharm list for Neuro Exam 4 Deck (54)
Loading flashcards...
1

Chlorpromazine

"Typical" First Generation Anti-Psychotic

Schizophrenia

Blockade of D2 receptors explains most significant pharmacological effects of antipsychotics, though these drugs also blocks other Dopamine 5HT, alpha-1, muscarinic, and histamine receptors

D2>5HT = good against POSITIVE symptoms

ADVERSE: ANS symptoms (Dry mouth, tachycardia, constipation, orthostatic hypotension, etc) and Sedation (Musc and Hist block)
High lipid solubility; passes into CNS and will cross placenta and exert effects on fetus

2

Haloperidol

"Typical" First Generation Anti-Psychotic

Schizophrenia
Treat stimulant-induced psychosis

Blockade of D2 receptors explains most significant pharmacological effects of antipsychotics, though these drugs also blocks other Dopamine 5HT, alpha-1, muscarinic, and histamine receptors

D2>5HT = good against POSITIVE symptoms

ADVERSE: Effects associated with D2 block, including acute dystonia, akathisia, Pseudoparkinsonism, and tardive dyskinesia
High lipid solubility; passes into CNS and will cross placenta and exert effects on fetus

3

Clozapine

"Atypical" Second Generation Anti-Psychotic

Schizophrenia

5HT2A> D2= good against
negative symptoms

Causes less psuedoparkinsonism

ADVERSE: Agranulocytosis, Weight gain, Altered thermoregulation, Phtosensitivity, Lowered seizure threshold Neuroleptic malignant syndrome
High lipid solubility; passes into CNS and will cross placenta and exert effects on fetus

4

Quetiapine

"Atypical" Second Generation Anti-Psychotic

Schizophrenia
Bipolar Depression

5HT2A> D2= good against
negative symptoms

ADVERSE: Weight gain, Altered thermoregulation, Phtosensitivity, Lowered seizure threshold Neuroleptic malignant syndrome
High lipid solubility; passes into CNS and will cross placenta and exert effects on fetus

5

Fluoxetine

Selective Serotonin Reuptake Inhibitors (SSRIs)

Blocks SERT, preventing reuptake of 5HT
Safe, multiple indications: GAD, Social anxiety, Panic, OCD, PTSD, PDD

ADVERSE:
*Acute: diarrhea, nausea, jitters/anxiety, dry mouth, P450 inhibition
*Delayed: sexual side effects, weight gain, cognitive blunting
*Death with overdose is rare; withdrawal=flu-like symptoms
*SSRIs+MAOIs = serotonin syndrome (hyperthermia, rigidity, confusion, HTN)

*Note: Olanzapine+fluoxetine used for Bipolar depression

6

Paroxetine

Selective Serotonin Reuptake Inhibitors (SSRIs)

Blocks SERT, preventing reuptake of 5HT
Safe, multiple indications: GAD, Social anxiety, Panic, OCD, PTSD, PDD

ADVERSE:
*Acute: diarrhea, nausea, jitters/anxiety, dry mouth, P450 inhibition
*Delayed: sexual side effects, weight gain, cognitive blunting
*Death with overdose is rare; withdrawal=flu-like symptoms
*SSRIs+MAOIs = serotonin syndrome (hyperthermia, rigidity, confusion, HTN)

7

Esciralopram

SSRI

8

Bupropion

Aka Wellbutrin

Nicotinic receptor antagonist/DA reuptake inhibitor

Treatment for:
*Nicotine addiction
*Stimulant (cocaine, meth, nicotine, MDMA) withdrawal
*Depression
*ADHD

9

Venlafaxine

Serotonin-Norepinephrine Reuptake Inhibitors (SNRI)

Block NET and SERT, preventing reuptake of Norepi and 5HT

Better tolerated than TCADs, multiple indications

ADVERSE: Sexual side effects, seating, increased diastolic blood pressure, withdrawal syndrome (flu-like, “electric shocks”) from missed doses, More rapid appearance of withdrawal than SSRIs
Specific to Venlafaxine: HTN, anxiety

10

Trazadone

Mixed Antidepressant
Insomnia treatment (with non-GABA action)

Complex 5HT mech

Can cause drowsiness

11

Amitriptyline

Tricyclic Antidepressants

Block NET and SERT, preventing reuptake of Norepi and 5HT

Time tested, very effective esp. in severe depression, can monitor blood levels

Now SECOND line for depression

Can be used in insomnia

ADVERSE: Hypotension, weight gain, sexual side effects, anticholinergic effects (constipation, dry mouth, etc), sedation, dangerous in overdose (arrhymias, seizures)

12

Phenelzine

Monamine Oxidase Inhibitors

Inhibit MAO, which degrades dopamine
Effective in non-responsive patients, especially atypical depression

ADVERSE: Postural hypotension, weight gain, sexual side effects, anticholinergic effects
Hypertensive crisis—Tyramine reaction (eating foods rich in tyramine such as
sausage, aged cheese, wine can provoke HTN attack)
Seizures, shock, hyperthermia in overdose

13

Lithium carbonate

Best studied, best proven drug for MANIA
Anti-mania, some antidepressant and anti-suicidal. BEST preventative agent for mania

Can be used in bipolar depression, but is least affective out of other agents

Thought to interfere with recycling of phosphoinositides= decrease action of GPCRs; may be involved in genes for growth factors/neuronal plasticity

ADVERSE: Tremor, nausea, diarrhea, taste, thirst, cognitive dulling, narrow therapeutic window, renal effects, diabetes insipidus, hypothyroidism. Diuretics can decrease renal clearance=higher plasma levels of Li
NSAIDs can also increase plasma Li

14

Alpraxolam

Benzodiazepine

CYP450 phase I and II >> renal excretion

Uses: Acute anxiety

15

Flurazepam

Benzodiazepine

Insomnia treatment, second line after "Z" drugs.

Anti-anxiety

Bind alpha 1 AND alpha 2/5 GABA receptors >> sleep AND anxiolysis
Facilitate process of GABA opening, but does NOT initiate chloride current (unlike barbs)

(long): half-life=75-90 hrs with active metabolite

ADVERSE: can accumulate due to impaired hepatic clearance, leading to daytime sedation/overdose. BLACK BOX: strange sleep behavior / severe allergic rxns Combined CNS depression (i.e. with EtOH); sedation; tolerance Dependence (Schedule IV)
Rebound insomnia with abrupt discontinuation

Treat toxicity with flumazenil (bdz antagonist)

16

Diazepam

Benzodiazepine

Enhance GABA activity

Lipid soluble, can pass into CNS

Metabolized via CYP450, then renal excretion

Treats:
*Seizures; status epilepticus (can develop tolerance)
*Seizures from stimulant overdose
*Anxiety (rapid, can be used prn)

IV anesthesia adjunct for anxiety

Toxicity is common; death from toxicity is NOT
ADDITIVE effects with other CNS depressants

Dependence (Schedule IV)

17

Oxazepam

Benzodiazepine

Enhance GABA activity

Lipid soluble, can pass into CNS

NOT P450 metabolized—good for elderly and in liver impairments

Uses:
*Anticonvulsant
*Anxiolytic
*Muscle relaxant

Toxicity is common; death from toxicity is NOT
ADDITIVE effects with other CNS depressants

Dependence (Schedule IV)

18

Triazolam

Benzodiazepine

Rapid absorption, can be used prn

Uses:
*Anxiolytic
*Muslce relaxant

Toxicity is common, death from toxicity is NOT. Can have additive effects with other CNS depressants

Dependence (Schedule IV)

19

Midazolam

Benzodiazepine

Enhance GABA activity

Lipid soluble, can pass into CNS

CYP450 metabolism then renal excretion

Uses:
*Anticonvulsant
*Anxiolytic
*Muscle relaxant

Toxicity is common; death from toxicity is NOT
ADDITIVE effects with other CNS depressants

Dependence (Schedule IV)

20

Lorazepam

Benzodiazepine

Enhance GABA activity

Lipid soluble, can pass into CNS

NOT P450 metabolized—good for elderly and in liver impairments

Uses:
*Anticonvulsant
*Anxiolytic
*Muscle relaxant

Toxicity is common; death from toxicity is NOT
ADDITIVE effects with other CNS depressants

Dependence (Schedule IV)

21

Temazepam

Benzodiazepine

Treat insomnia

Bind alpha 1 AND alpha 2/5 GABA receptorssleep AND anxiolysis

Facilitate process of GABA opening, but does NOT initiate chloride current (unlike barbs)

Intermediate half-life=9-13 hrs

BLACK BOX: strange sleep behavior / severe allergic rxns Combined CNS depression (i.e. with EtOH); sedation; tolerance Dependence (Schedule IV)
Rebound insomnia with abrupt discontinuation

Treat toxicity with flumazenil (bdz antagonist)

22

Flumazenil

Antagonist at the benzodiazepine binding site, reverses the CNS effects of benzodiazepines

23

Zolpidem (Ambien)

"Z drug" of Insomnia treatment; first line treatment!

Bind gamma subunit to facilitate process of GABA opening, but does NOT initiate chloride current (unlike barbs)

Bind alpha 1 GABA receptors >> sleep without anxiolysis

Short half life; good for "I can't fall asleep!"

BLACK BOX warning for all BDZ-site binding GABA agonists >> strange sleep behavior and severe allergic reactions
Schedule IV
Many have some drowsiness, dizziness, headache

24

Eszopiclone (Lunesta)

"Z drug" of Insomnia treatment; first line treatment!

Bind gamma subunit to facilitate process of GABA opening, but does NOT initiate chloride current (unlike barbs)

Bind alpha 1 GABA receptors >> sleep without anxiolysis

Longer half life, more for long-term use (little to no tolerance)

BLACK BOX warning for all BDZ-site binding GABA agonists >> strange sleep behavior and severe allergic reactions
Schedule IV
Many have some drowsiness, dizziness, headache

25

Zaleplon (Sonata)

"Z drug" of Insomnia treatment; first line treatment!

Bind gamma subunit to facilitate process of GABA opening, but does NOT initiate chloride current (unlike barbs)

Bind alpha 1 GABA receptors >> sleep without anxiolysis

Short half life for duration of 6-8 hours; good for "I can't stay asleep!"

BLACK BOX warning for all BDZ-site binding GABA agonists >> strange sleep behavior and severe allergic reactions
Schedule IV
Many have some drowsiness, dizziness, headache

26

Phenobarbital

Barbiturate

Enhance GABA, decrease GLU

Classic CYP450 inducer

Used mostly in neonatal status epilepticus. Sometimes add-on for seizures but sedation limits use

Used to be used as anxiolytic agent, but not really anymore because abuse potential

ADVERSE: CYP450 = DDIs, Sedation, irritability, interferes with learning

27

Ramelteon

Insomnia treatment

Non-GABA Action

Agonist at melatonin MT1 (induce sleepiness) and MT2 receptors (regulation
of circadian rhythms) in suprachiasmatic nucleus of hypothalamus. Decreases mean latency to sleep.

ADVERSE: Dizziness, somnolence, fatigue, nausea; 5% incidence or less.

28

Diphenhydramine

Antihistamines

H1 histamine and muscarinic antagonist

May be effective in short term treatment of insomnia
Heavily advertised but NOT recommended

Antimuscarinic effects can be troublesome in elderly

29

Cocaine

Stimulant

DAT (+SERT, NET)

Toxicity=sympathetic sx (high BP, high temp, sweating)

Treat with supportive measures (ventilation, lavage, etc)

Treat seizures with Diazepam

Treat high BP (DBP>120) with phentolamine  DON’T use beta-blockers (unopposed alpha-stimulation)

Treat psychosis with haloperidol

Withdrawal is generally mild (mostly craving, depression, sleepy). Treat with TCADs, bupropion

30

Amphetamine

1. Stimulant (think cocaine)
DAT (+SERT, NET)
Can stimulate psychosis
Amphetamine salts = Adderall = ADHD tx



2. "ampehtamine-like" Hallucinogen
5HT-2A receptor (Gq) partial agonist

31

Methamphetamine

Stimulant
DAT (+SERT, NET)

Toxicity=sympathetic sx (high BP, high temp, sweating)
Treat with supportive measures (ventilation, lavage, etc)
Treat seizures with Diazepam
Treat high BP (DBP>120) with phentolamine  DON’T use beta-blockers (unopposed alpha-stimulation)
Treat psychosis with haloperidol

Withdrawal is mild (craving, depression, sleepy)

32

Nicotine

Stimulant
Nicotinic Receptor


Toxicity usually due to accidental ingestion (i.e. of tobacco products (kids), of nicotine insecticides)
Toxicity=nausea, vomiting, stomach pain, salivation, diarrhea, headacheprogress to hypotension, convulsions, resp failure
Treat with supportive measures (ventilation, lavage, etc)
Individual with impaired nicotine metabolism=protection=less likely to become addicted to cigarettes
Increased use in anxiety, VERY common in Schizophrenia

Withdrawal: irritable, anxiety, depression, restless, increased appetite. Treat with nicotine replacement therapy like bupropion

33

Alcohol

CNS depressant
Increase GABA-A, decrease NMDA

Withdrawal:
Increased DTR (deep tendon reflex), BP and pulse
Seizures (1-2 days)
Delirium Tremors (2-5 days)

Treatment Meds:
Disulfiram (inhibits acetaldehyde dehydrogenase)
Naltrexone: opioid antagonist
Acamprosate (GABA antagonist)

NADH is produced via ETOH metabolism, which depletes the NAD required for oxidative reactions Leads to increased blood lactate (acidosis), increased Mg excretion (convulsions), decreased uric acid excretion (gout attack), increase acetyl CoA (inc fatty acid synthesis and decrease fat breakdown= fatty liver), decrease krebs=decreased gluconeogenesis (hypoglycemia)

Increased use in anxiety
3rd leading cause of death

34

Barbiturates

CNS Depressant

Increase GABA-A, decrease NMDA

Act via prolonging GABA channel chloride effect even in absence of GABA (at high concentrations) and decreasing Glutamate

Toxicity: respiratory depression, hypotension, coma, death

*High tolerance*

Withdrawal carries significant risk of morbidity/mortality: treat with reduced dose or substitution therapy and monitor for seizures

**Classic inducers of CYP450**

Uses: Not often used in anxiety anymore, Insomnia,

35

Benzodiazepines

CNS Depressant

Increase GABA-A only
Bind alpha 1 AND alpha 2/5 GABA receptors >> sleep AND anxiolysis
Facilitate process of GABA opening, but does NOT initiate chloride current

Toxicity: respiratory depression, hypotension, coma, death

Benzo antagonist: flumazenil

Withdrawal carries significant risk of morbidity/mortality: treat with reduced dose or substitution therapy and monitor for seizures. Delirium Tremors. Increased DTR, BP and Pulse

Uses:
Panic Disorder, GAD, Social Phobia, Anxiolytic agent, Insomnia medication, Absence seizures

36

Heroin


Mu-opioid receptor (Gi/o) agonists

Acute toxicity= coma, respiratory depression, pin-point pupils

Tolerance develops to most opioids (not equally for all systems i.e. develop little tolerance to constipation) Dependence develops rapidly; withdrawal sx can be intense but are not medically dangerous

Withdrawal treatment: clonidine (for symp sx); methadone (to alleviate sx), buprenophine (partial agonist)

37

Marijuana

B-1 receptor (Gi/o) agonist

Intoxication: Slowed time, decreased coordination, euphoria.

Toxicity: severe overdose is rare, but can have paranoia, memory impairment, tremors, high HR, dec. strength and coordination>> should not drive

Can exacerbate sx of existing psychotic illness Treat with supportive measures

ADVERSE: Long-term use can cause cognitive impairment, “amotivational syndrome,” pulm problems (COPD, laryngitis, pharyngitis)
Tolerance develops and disappears rapidly; high potential for dependence
Mild withdrawal=sleep issues, anorexia, irritability, cravings

38

Methadone

Opiod

Mu-opioid receptor (Gi/o) agonists

Use in opiod withdrawal to alleviate sx

Acute toxicity= coma, respiratory depression, pin-point pupils

Treat toxicity with naloxone

39

Buprenorphrine

Treatment for Opiod addiction

Partial agonist at mu opioid receptors that produces minimal withdrawal symptoms, has a low potential for overdose toxicity, a long duration of action, and will block the acute reinforcing effects of heroin. Do not experience the ups and downs of heroin
and drug craving diminishes and may disappear

40

Clonidine

Alpha Agonists

Uses:
*ADHD treatment
*Opiod withdrawal
*Alcohol withdrawal

In treating withdrawal: will alleviate symptoms of sympathetic nervous system overactivity (nausea /vomiting, cramps, sweating, tachycardia, and increased blood pressure) that occur during acute
withdrawal

41

Disulfiram

Inhibits acetaldehyde dehydrogenase

Results in 5-10 fold increase in acetaldehyde levels (nausea/vomiting, respiratory and cardiovascular collapse, convulsions)

EtOH sensitizing drug

Alcohol addiction treatment

42

Naltrexone

Opioid antagonist

Medication for Alcohol and Opiod addiction

Alcohol: Shown to reduce alcohol craving, consumption, and relapse rates when used in combination with psychotherapy

Opiods: block reinforcing actions of
heroin but has no effect on craving or the PWS

43

d-Ampethamine

x

44

Methylphenidate

Stimulant

Aka Ritalin

Treatment for ADHD

Block reuptake pump and/or increase release of norepinephrine, but these drugs also block dopamine reuptake and/or increase dopamine release, leading to high abuse potential

45

Nitrous oxide

Volatile Anesthetics

Only true gas (other are volatile liquids); MAC is 105% so can’t be sued as a sole anesthetic (combine with barb+opioid)
Concentration effect: because of high inspired %, uptake rate is faster than predicted
Diffusion hypoxia: when admin is terminated, large volume of nitrous oxide leaves blood and expands lungsdiutes alveolar O2 >> hypoxia
Second gas effect: if combined with another gas, the huge uptake of rate of nitrous oxide also pulls second gas, so second gas has faster uptake than
expected

46

Halothane

Volatile Anesthetics

fluorinated hydrocarbon

Highly potent, poor analgesic (used to be widely used, not so much anymore)

ADVERSE: Respiratory and cardiovascular failure (arrhythmias), Hepatotoxic (1/10,000 have fever/anorexia/nausea 2-5 days later and 50% of these patients die; repeated exposure significantly increases risk)
Malignant hyperthermia (occurs with most volatile GAs): muscle rigidity and fever (due to mutation in RyR)

47

Dantrolene

Causes relaxation by blocking Ca2+ release via the ryanodine receptor

Treatment for malignant hypothermia (plus an ice bath)

48

Phenytoin

Inhibit VSSC (Na channel) in use-dependent manner; suppress repetitive APs

For partial seizures and gen tonic-clonic
Fosphenytoin (water soluble pro drug) for
active seizures
NO LONGER FIRST LINE b/c of variable
kinetics and availability of better drugs

ADVERSE: Strong P450 inducer!
Nystagmus, diplopia, ataxia, sedation, rash, gingival hyperplasia. Long term=osteomalacia/peripheral neuropath

49

Carbamazepine

Inhibit VSSC (Na channel) in use-dependent manner; suppress repetitive APs

Drug of choice for partial seizures
Often tried first for generalized tonic-clonic

ADVERSE: P450 inducer. Can cause Diplopia, ataxia, nausea/vomiting, drowiness, occasionally Hypnatremia, Risk of Steven-Johnson syndrome

50

Levetiracetam

Treats tonic-clonic seizures, Atypical Absence seizures, Atonic or Myoclonic seizures

Binds to and inhibits function of synaptic vesicle protein SV2A in Ca++-
mediated neurotransmitter release. Relation to antiseizure action is uncertain

51

Valproate

Treats tonic-clonic seizures and Atypical Absence seizures

Blocks VSCC

Increases levels of other anti-seizure drug, Lamotrigine


Risk of birth defects; mothers need to take higher doses of folic acid

52

Divalproex

Anti-maniac, Anti-seizures

Mechanism of Action: Unclear, but probably involves some potentiation of GABA function (weak effect on GABA-transaminase) and effects on membrane excitability (similar to phenytoin). Limits activity of Ttype
Ca++-channels.

ADVERSE: Not proven as preventative agent, weight gain, sedation, “perming effect”—hair gets frizzy and/or falls out

53

Ethosuximide

Anti-seizure Drug

Inhibit low-threshold T-type Ca channel

Complete oral absorption
CYP3A4 metabolized

Drug of choice for ABSENCE SEIZURES

ADVERSE: CYP3A4 inducing/inhibiting DDIs
GI upset (dose-dependent); some HA, dizziness

54

Treatment efficacy for bipolar depression

quetiapine> lamotrigine> olanzapine+fluoxetine>lithium