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Pharmacology > CNS > Flashcards

CNS Flashcards

1
Q

Drugs that block D2 receptors in vomiting center

A
  1. Metoclopramide - crosses BBB
  2. Domperidone - does not cross BBB + L-dopa
  3. Chlorpromazine and promethazine
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2
Q

Drugs that block D2 receptors in basal ganglia

A
  1. L-dopa
  2. Bromocriptine
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3
Q

Drugs that block D2 receptors in pituitary gland

A
  1. Bromocriptine
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4
Q

Classification of anti-psychotic drugs

A

Typical older generation drugs
مشينا الprom ولاقانا dro وthixene قالو لينا halo
1. Phenothiazine - chlorpromazine and promethazine
- zine chlorprom + prometh
2. Butyrophenones - haloperidol and droperidol
dro بقول ليك halo -peridol
3. Thioxanthene - thiothixene and chlorprothixene
thiothix + chlrorpro - thixene

Atypical newer drugs
ROC
1. Risperidone
2. Olanzapine
3. Clozapine - resistant cases

risperiodone and zapine zap the crazy patient

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5
Q

Therapeutic uses of antipsychotic drugs

A
  1. Schizophrenia and mania - immediate quotienting reaction; full effect 1-2 weeks later
  2. Prevent severe nausea and vomiting due to cancer chemotherapy and radiation treatment - chlorpromazine and promethazine
  3. Chlorpromazine
    - Intractable hiccups
    - Hypothermia as an anesthetic adjuvant

Chlorpromazine
1. Prevent nausea and vomiting
2. Intractable hiccups
3. Anesthetic adjuvant

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6
Q

Adverse effects of antipsychotic drugs

A
  1. Extrapyramidal manifestations / parkinsonism like syndrome older
    Blocks D2 in basal ganglia
    - Tremors
    - Dystonia
    - Dyskinesia
  2. Neuroleptic malignant syndrome
    Autonomic disturbance
    - Hypertension
    - Muscle rigidity
    - Hyperthermia
    - Sweating
    - Convulsions
    Serious complication 20% mortality rate
  3. Autonomic disturbance
    - Blocks α receptor - postural hypotension and sexual dysfunction
    - Muscarinic block - atropine like action
  4. Endocrine disturbance atypical
    - Pituitary gland - hyperprolactinemia amenorrhea and gynecomastia
    - Increased hunger - weight gain and diabetes (5HT2A receptors responsible for satiety)
  5. Arrhythmia - sudden cardiac arrest
  6. Cholestatic jaundice especially chlorpromazine
  7. Agranulocytosis especially clozapine atypical
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7
Q

Parkinsonism

A

Progressive degenerative disorder of the nigrostiral pathway resulting in decreased dopamine (imbalance between dopamine inhibitory an dactelycholine excitatory) which manifests as
Motor manifestations
1. Muscle rigidity
2. Bradykinesia and shuffling gate
3. Tremors at rest
Non-motor manifestations 3Ds
1. Dementia
2. Depression
3. Disturbance of sleep

Risk factors
1. Age >60 (early onset dementia)
2. Head trauma
3. Insecticides

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8
Q

Classification of antiparkinsoian durgs

A

Dopaminergic drugs ↑ dopamine
1. L-dopa + tolcapone (COMT inhibotr) + selegiline (MAO B) + carbidopa
2. Bromocriptine (partial dopaine angonist بحل مكان الlevodpa)
3. Amandine (infuanzea A dopamine release)

Anti-cholinergic ↓ Ach
BOT
1. Benztropine (علي وزن atrophine)
2. Orphenadrine
3. Trihexyphenidyl

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9
Q

Levodopa - L-dopa

A

Pharmacokinetics
- Absorption - well absorbed from GIT; taken orally; take on an empty stomach leucine and isoleucine interfere with absorption
L L levodopa leucine
- Short half life 1-2 hrs → COMT tolcapone and MAO B inhibitors seligium
Short half life → on and off phenomenon
- >90 % of L-dopa decarboxylation in peripheral tissue → peripheral decraboxylase enzymes crabidopa and benserazide

Mechanism of action
L-dopa decarboxylation dopamine

Adverse effects
GIT 1
1. Vomiting center → nauseas and vomiting
CNS 2
2. Mesolimbic and mesocortical tract → mood changes, hallucination and nightmares
3. On-off phenomenon - sudden improvement followed by sudden immobility
4. Dyskinesia
Autonomic 3
5. Postural hypotension
Fenoldopam antihypertensive vasodilation D1 receptors
L-dopa
60% peripheral → D1 receptors → vasodilation
20% brain
6. Sympathomimetic → arrythmia + mydriasis increases IOP
7. Brown urine and sweat due to homovanillic acid metabolite

Interactions
DO NOT
1. Give on an empty stomach - interacts with leucine and isoleucine
2.Vitamin B6 pyridoxine ↑ peripheral decarboxylation
3. Antipsychotic drugs - decrease dopamine
GIVE
4. COMT inhibitor + MAO B inhibitor + peripheral decarboxylase inhibitor

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10
Q

COMT inhibitor

A
  1. Tolcapone
  2. Entacapone

Inhibits COMT enzyme reversibly to increase half-life
L-dopa → L-3-methyldopa in gut and liver

Side effects
1. Acute fulminant hepatitis acute liver failure
2. L-dopa - nauseas, vomiting hallucinations, mood swings

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11
Q

Selective MAO B inhibitor

A
  1. Selegiline

Inhibits dopamine breakdown in brain by MAO B
DOES NOT cause cheese reaction
- Cheese reaction happens in MAO A inhibitors in the liver they prevent tyramine breakdown (found in cheese) which enters the circulation and causes increased BP and acute hypertensive crisis

Side effects
1. Insomnia IS
2. L-dopa - nauseas, vomiting hallucinations, mood swings

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12
Q

Domapine agonists

A
  1. Bromocreptine

Ergot alkaloid
Can cross BBB and absorbed easilty

Advantages
Long half-life - do not need MAO or COMT inhibitors AND no on and off phenomenon

Side effects
1. Pulmonary fibrosis
2. L-dopa - nauseas, vomiting hallucinations, mood swings, postural hypotension

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13
Q

Dopamine release

A
  1. Amantadine

Uses
1. Infulenza A
2. Antiparkinsoin

Mechanism of action
1. Increases dopamine release
2. Decreases dopamine reputpake
3. Direct effect on dopamine receptors

Side effects
1. Levido reticularis - skin pigmentation/moltted skin
2. L-dopa - nauseas, vomiting hallucinations, mood swings

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14
Q

Anticholingeric drugs

A

BOT
1. Benztropine
2. Orphenadrine
3. Trihexyphenidyl

Blocks M1 central receptors

Effects
1. Improvement of tremor
2. Prevent sialorrhea
3. Control acute drug induced extrapyramidal manifestations

Side effects
1. Dementia
2. Urine retention especially with BPH
3. Narrow angle glaucoma
SAD HC
زغلوله االناشفه حبست جوزها ابو سريعه

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15
Q

Depression

A

Mood distrubance

Pathophysiology
1. Genetics - 4 genes
2. Biogenic amine and receptor theory
- ↓ NA ↓ serotonin ↓ dopamine
- Upregulation of 5HT2A and 5HT2c receptors
3. Neurotrophic and cytokine theory
- ↓ BDNF (brain derived neurotrophic factor)
- Hypothalamic-pituitary axis dysfunction
- Proinflammatory cytokines IL1, IL6 and TNF

Types of depression
1. Unipolar - MDD major depressive disorder constant low levels
2. Bipolar - Manic depressive depression high and low levels
Mood stabilizer

Symptoms
Emotional serotonin
1. Anhedonia
2. Apathy and low self esteem
3. Loss of motivation
Psychosomatic/biologic NA
1. Chronic pain
2. Sleep disturbance
3. Loss of appetite and libido (does not want to eat)

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16
Q

Classification of antidepressant drugs

A
  1. MAOIs - Selegiline, phenelzine, tranylcypromine, Moclobemide
    TPS
  2. TCAs - Imipramine, Desipramine, Clomipramine, Amitriptyline, Nortriptyline
    - pramine imi, desi and clomi
    - triptyline ami and nor
  3. SSRIs - Fluoxetine, Paroxetine, Sertraline MI, Citalopram, Escetalopram
    - oxetine flu and par
    - line sertra
    - lopram cita and esceta
  4. Atypical heterocyclic antidepressants - venlafaxine, duloxetine, trazodone and mirtazapine
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17
Q

MAOIs

A

Mono amine oxidase inhibitors
TPS
1. Tranylcypromine hepatotoxic
2. Phenelzine hepatotoxic
3. Selegiline antiparkinsonian

Inhibit MAO A and therefore lead to accumulation of NA and serotonin inside the neuron
- Most are irreversible - recovery takes few weeks
- Moclobemide is reversible
Effect takes place after 2-3 weeks to allow for accumulation

2 types of MAO
MAO A → cytoplasm of neurons + liver
- Non-specific NA, dopamine and serotonin
MAO B → CNS
- dopamine only

Therapeutic uses
1. Major depression unresponsive to other drugs
clinical improvement of all anti-depressive drugs needs 2-3 weeks
2. Antiparkinsonians selegiline

Side effects
1. Postural hypotension
- All drugs that cause dysregulation in brain neurotransmitters cause hypotension
- ↑ NA works on α2 autoinhibitory receptors decrease vasodilation decrease BP
2. Sexual dysfunction - delayed orgasm
premature ejaculation
3. Serotonin syndrome - MAOIs + TCAs/SSRIs
Autonomic dysfunction HHHM
- Hyperthermia
- Hypertension
- Headache
- Sweating
- Muscle rigidity
- Arrhythmia - tachycardia
4.CNS stimulation
- Insomnia
- Convulsions
- Irritability
- Tremors
- Hyperthermia
5. Cheese reaction - hypertensive crisis
Diary products contain tyramine which gets into the circulation and increases BP causing hypertensive crisis

18
Q

TCAs

A

Tricyclic antidepressants

  1. Imipramine
  2. Clopramine
  3. Desipramine
  4. Amitriptyline
  5. Nortriptyline

-pramine family
Imi, clo and desi
-triptyline family
Ami and nor

Inhibit NA and serotonin reuptake transporters leading to accumulation of NA and serotonin in the tissue
inhibition of amine pump

Therapeutic uses
1. Major depressive disorders
2. Chronic pain fibromyalgia, neuropathic pain and migraine prophylaxis
3. Nocturnal enuresis in children imipramine

Adverse affects
1. Same as MAOIs → postural hypotension, sexual dysfunction and serotonin syndrome
2. CNS sedation
3. Atropine like action
4. Cardiac arrythmia
TCA toxicity
Manifestations
- Atropine like actions
- Metabolic acidosis
- Tachycardia + wide QRS complex + prolonged QT

Treatment
1. IV NaCO3 - solves metabolic acidosis
2. IV lidocaine

Do not put on dialysis since TCAs have large volume distribution

19
Q

SSRIs

A

Selective serotonin receptor inhibitors

  1. Fluoxetine
  2. Paroxetine
  3. Sertraline MI
  4. Citalopram and escitalopram

5 stars
- oxetine family flu and par
- sertraline line MI dead straight line
- pram family citalopram and escitalopram

Inhibit serotonin reuptake transporters leading to the accumulation of serotonin in the neuronal tissue

Less side effect than TCAs

Therapeutic uses
1. Major depressive disorders
2. OCD
2. GAD
Benzodiazepines - tolerance and addiction
OLAAAAAAAAAAA

Side effects
1. Same as MOAIs - postural hypotension, sexual dysfunction and serotonin syndrome
2. Either CNS sedation or stimulation - tolerance develops over time goes away
3. GIT irritation - use PPIs
4. Arrythmia (not as much as TCAs) - increase QT

For acute MI use Sertraline
Stop SSRIs gradually over 4 weeks

20
Q

Atypical heterocyclic antidepressants

A

Partial reuptake inhibitors
NA 20 %
Serotonin 30%
VD
1. Venlafaxine
2. Duloxetine diabetic autonomic neuropathy

Receptor blockers
Block 5HT2A and 5HT2C receptors
TM
1. Trazodone
2. Mirtazapine

21
Q

Drugs that block NA or serotonin

A

TCAs - block both NA and serotonin
SSRIS - block serotonin
Atypical - block NA 20% and serotonin 30%

22
Q

Classification of anti-epileptic drugs

A

First generation
1. Phenytoin
2. Carbamazepine
3. Valproic acid
4. Ethosuximide
5. Phenobarbital
6. Benzodiazepam

  • Increase GABA
  • Block Na+ channel
  • Block T-type Ca2+ channel

More side effects

Second generation
1. Vigabatrin
2. Lamotrigine
3. Topiramate
4. Levetiracetam
5. Gabapentin and pregabalin
6. Tiagabine

Excitatory neurotransmitters
- Decrease glutamate and aspartate
- Block NDMA or AMPA

Less side effects

23
Q

Phenytoin

A

Blocks Na+ channels in brain and heart

Therapeutic uses
1. Type 1B antiarrhythmic drug
2. Tonic clonic seizures (partial and generalized seizures)
3. IV fosphenytoin status epilepticus

Adverse effects
1. CNS → NDA nystagmus, diplopia and ataxia
2. Liver → increases microsomal enzyme induction
3. Blood → megaloblastic anemia - increased folic acid destruction
4. Teratogenic → craniofacial abnormalities and spina bifida
5. Gingival hyperplasia
6. Lymphadenopathy and splenomegaly
7. Hirsutism
8. Osteomalacia - increased vitamin D metabolism
9. Hepatoxicity

24
Q

Common adverese effects of first genetration anti-epipleitc drugs

A
  1. CNS → NDA nystagmus, diplopia nad ataxia
  2. Liver → increased microsomal enzyme induction
  3. Blood → megaloblastic anemia - increases folic acid metabolism
  4. Teratogenic
    - Craniofacial abnormalities fetal hydantoin syndrome → microcephaly, no nose bridge, cleft palate and atrophied distal phalanges
    - Spina bifida - neural tube defect due to folic acid metabolism
    Take folic acid
25
Q

Carbamazepine

A

Blocks Na+ channels in brain only

Therapeutic uses
1. 1st line in focal seizure
2. 2nd line in tonic clonic seizures (partial and generalized seizures (grand mal epilepsy)
3. Trigeminal neuralgia

Adverse effects
1. Same as phenytoin → NDA, increases microsomal enzyme induction, megaloblastic anemia and bone depression and teratogenic
2. ** Increases ADH secretion** edema, hyponatremia and CHF

Autoinduction

26
Q

Valproic acid (Depakene)

A

Mixed mechanism
1. Increases GABA → inhibits GABA transaminase
2. Blocks Na+ channels
3. Blocks Ca2+ channels → absence seizures

Therapeutic uses
All types of epilepsy

Adverse effect
1. Same as phenytoin → NDA and most teratogenic
2. Microsomal enzyme inhibition
2. ** Alopecia**
3. Pancreatitis + fulminant liver hepatitis (COMT inhibitors)

MOST TERATOGENIC

27
Q

Hirsutism
Alopecia

A

Phenytoin - hirsutism
Valproic acid - alopecia

28
Q

Ethosuximide (Zarontin)

A

رحمه ربنا لي الشفع

Block T-type Ca2+ channels only in thalamocortical neurons

Therapeutic uses
1. 1st line for absence seizures

Adverse effects
1. GIT upset
2. Headache and dizziness

Least teratogenic drug

29
Q

Most and least teratogenic drugs

A

Most valproic acid
Least ethosuximide

30
Q

Phenobarbital

A

Increases GABA
1. Allosteric modulation of GABA A recepotrs
2. GABA agonist - gaba like action

Theraputic uses
1. Tonic clonic seziures
2. Status epilipticus

Adverse affects
1. Same as phenytoin → NDA, increases microsomal enzyme induction, megaloblastic anemia and bone depression and teratogenic
2. Tolerance + dependance
3. Respiratory depression in toxic doses

LIMITED USE DUE TO SIDE EFFECTS - SEDATIVE

31
Q

Status epilepticus

A
  1. Benzodiazepine - 1st line
  2. Fospheyntoin
  3. Phenobarbital
32
Q

Benzodiazepine

A

Increases GABA
- Allosteric modulation of GABA receptors

Therapeutic uses
1. 1st line
- Status epilepticus - diazepam
- Febrile seizures
2. Absence not so much - clonazepam

Adverse effects
1. Tolerance and dependence
2. Memory disturbance

LIMITED USE DUE TO SIDE EFFECTS

33
Q

Lamotrigine

A
  1. Blocks Na+ channels and voltage dependent Ca2+ channels
  2. Decreases glutamate release

Therapeutic uses
All
Might replace carbamazepine in focal

Adverse effects
1. Steven Johnson syndrome - high risk if combined with valproic acid
2. Insomnia

Preferred in pregnancy least teratogenic effect

34
Q

Tiagabine

A

Inhibits GABA reuptake into glial and other neurons therefore increases GABA concentration

Therapeutic uses
Adjuvant in focal seizure

Adverse effects
1. GIT upset
2. Dizziness

35
Q

1st line in
1. Focal seizures
2. Absence seizures
3. Status epilepticus and febrile
4. All

A
  1. Focal seizures - carbamazepine
  2. Absence seizures - ethosuximide
  3. Status epilepticus and febrile - benzodiazepine
  4. All - valproic acid
36
Q

Classification of opioids

A

Natural
1. Phenanthrene ring
- Morphine
- Codeine
- Bethain

CNS effects - addiction
* Spasmogenic*
Analgesics

  1. Benzyl isoquinoline ring
    papavrum and ine family
    - Papavarum
    - Noscapine
    - Narceine
    Papa no scaping narceine

Semi-synthetic
- Morphine
- Hydromorphone

Synthetic
1. Agonist
- Tramadol
- Meperidine family
- Methadone family
TMM

  1. Mixed
    Orphan pen and ephrine family
    - Butorphanol but orphan ol
    - Buprenorphine Bu pren orphine
    - Nalorphine
    - Nalbuphine
    - Pentzocin
  2. Antagonist
    xone family
    - Naloxone
    - Naltrexone
    N and x
    naloxone
    naltrexone
37
Q

Morphine

A

Natural plant alkolid phenanthanine dervied from opium plant pavapum soforinum

Pharmacokinetics
- Bioavailability → 25%
First pass metabolism + absorption
- HL → 4-5 hrs
- Metabolism → liver glucuronide conjugation active and inactive metabolites
- Excretion → 90% kidney 10% conjugated bile

Pharmacological effects
CNS 8
1. Analgesic except itching
MOA
1- Spinal analgesia - SGR dorsal horn in spinal cord inhibits substance P release
2- Supraspinal analgesia - descending inhibitory pain control
3- Decreases NA release in CNS
4- Stimulates opioid receptors in inflamed tissue decreases inflammatory mediators
2. Euphoria
3. Miosis pinpoint pupil - stimulates Edinger Westphal nucleus
4. Nausea and vomiting
5. Vagal stimulation - bradycardia
6. Cough suppression
7. Respiratory depression
8. Increased ICP - hypercapnia + vasodilation
CVS 2
1. Bradycardia → vagal stimulation no reflex tach
2. Postural hypotension → vagal stimulation + histamine release
Smooth muscle Spasmogenic
Bronchi
1. Bronchoconstriction - vagal stimulation + μ and δ receptor + histamine release

GIT
1. Constipation - μ increases segment non propulsive spasmodic movement + increases water absorption
Lomotil - loperamide + diphenoxylate + atropine treats constipation
Contraindicated in elderly with senile enlarged prostate

Gall bladder
1. Increases wall contraction and closes sphincter of oddi
Contraindicated in patients with gall stones

Gentourinary
1. Feeling of urgency with difficulty micturition
2. Prolonged labor - interferes with uterine contraction + cervical spasm

Therapeutic uses
1. Analgesic for severe pain - MI cancer and surgery
2. Acute pulmonary edema expect inferior MI - histamine release VD + pain relief + decreases tachypnea
3. Anesthesia adjuvant in big surgeries

In severe colic use atropine (spasmolytic and prevents vagal stimulation) + morphine

Adverse effects
CNS
1. Tolerance + dependence
2. Respiratory depression
3. Increased ICP
Eye
1. Severe miosis
CVS
1. Postural hypotension
2. Bradycardia
Bronchi
1. Bronchoconstriction
GIT
1. Biliary colic
2. Nausea
3. Constipation

Genitourinary
1. Feeling of urgency with difficult micturition
2. Prolonged labor

Contraindications
1. Asthmatic
2. Biliary colic
3. Elderly with senile prostatic enlargement
4. Inferior MI - vagal stimulation makes it worse
5. Liver failure - hepatic coma
6. Myxedema and hyperthyroidism - exaggerated response to morphine + also causes bradycardia
7. Hypovolemia, hypotension and bradycardia
8. Head trauma with increased ICP
9. Undiagnosed abdominal pain - masks pain
10. Extremes of age - greater risk of RD

38
Q

Morphine can treat all types of pain except itching. Why?

A
  1. Itching not pain
  2. Morphine causes histamine release
39
Q

Patient comes in with bradycardia and hypotension what are the differential

A
  1. Opioid overdose
  2. Beta blocker
40
Q

Side effects of anti-parkinsonian drugs

A
  1. L-dopa - brown urine and sweat homovanillic acid
  2. Tolcapone COMT inhibitor - fulminat hepatitis

Pharmacology (4 decks)

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