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Pharmacology FINAL (2nd sem) > A: 25-28 > Flashcards

A: 25-28 Flashcards

1
Q

Benzo’s MOA

A

Bind GABA-A receptor (BZ-binding site) > facilitate Cl- channel opening & increases frequency

  • membrane hyperpolarization
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2
Q

Benzos and DOA

A

super MaN is super fast
DC movies are super long
A is in the middle of mAn

T1/2= 2-40 hrs

Midazolam (oral, I.V) , Nitrazepam (oral)
Alprazolam (oral)
Diazepam (oral, IV) , Clonazepam (oral)

  • metabolism: hepatic conjugation
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3
Q

Benzo’s indication

A
  • Status epilepticus (diazepam)
  • skeletal m. relaxation ( diazepam)
  • absence and myoclonic seizure, infantile spasms (clonazepam)
  • bipolar disorder (clonazepam)
  • acute anxiety attack
  • panic attack
  • generalised anxiety disorder
  • Sleep problems

Not for major depression

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4
Q

Diazepam indicationns

A
  • Inducation of Anesthetia (IV)
  • Preoperative Sedation
  • treatment muscle spasticity : centrally acting skeletal Muscle relaxant
  • Anxiety, Panic and phobic disorders
  • Withdrawal state (ethanol, other sedative hypnotics) - because longer acting benzo
  • status epilepticus
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5
Q

Clonazepam indic.

A
  • Anxiety, panic & phobic disorders
  • Bipolar
  • Seizures

oral!

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6
Q

Benzo’s drug interaction

A

Antihistamines gen 1
Alcohol
Barb’s

  • Additive CNS dep occurs when sedative hypnotic are used with other drugs in the class
    • 1st gen antihistamine
    • Anti-pscychotics
    • opioid analgesics
    • tri-cyclic antidepressant
    • Barbiturate
    • alcohol
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7
Q

Alprazolam indications

A

oral

  • Anxiety, panic and phobic disorders
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8
Q

Nitrazepam indication

A

Nitra = NIGHT

oral

  • Sleep disorders
  • insomnia
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9
Q

Midazolam indication

A

oral, I.V

  • preoperative sedation
  • Anasthesia (iv)
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10
Q

Toxicities of benzos

A
  • Extension of CNS deppressant action
  • tolerance
  • dependence liability
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11
Q

Benzo’s antag.

A

Flumazenil (antagonist at BZ-specific binding site on GABA-A r)
-مازن-

also for zolpidem ocerdose

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12
Q

Non Benzo’s

A

Zaleplon, Zolpidem- (newer hypnotics) GABA-A agonist

  • binds to GABA-A receptor site
  • facilitates chloride chn opening and increase duration

Your BMR is up when you sleep well

Busiprone- 5HT partial agonist & possible D2-r Busi is prone to allergies
Melatonin-
Rameltone- Melatonine-r agonist.( activates MT1 & MT2 receptors in supra-chiasmatic nucleus) ram sleeps and dream on Elton

+ SSRI (selective serotonin reuptake inhibitors) : Fluoxetine , (ES) citalopram, Sertraline

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13
Q

flumazenil

administration, duration

toxicities

A
  • I.V
  • short T1/2
  • SE
    • Agitation
    • confusion
    • possible withdrawal syndrome
    • seizures
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14
Q

Zaleplon,

Zolpidem

indication, administration, pharmacokinetics

A
  • Sleep disorders esp when sleep onset is delayed
  • oral
  • P450 substrate
  • Short T1/2
  • additive CNS depression with ethanol and other CNS depressants
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15
Q

Zaleplon, zolpidem toxicities

A
  • Extension of CNS depressant effects
  • dependence liability ( less than that of benzos because withdrawal symtpms are minimal after sudden discontinuation
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16
Q

Ramelteon mechanism and indication

A

Activation MT1 & MT2 receptors in suprachiasmatic nucleus (melatonin-r agonsit)

  • Sleep disorders esp when onset of sleep is delayed ( same as zaleplon , zolpidem)
  • NOT a controlled substance
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17
Q

Ramelteon administration, metabolism , toxicities

A
  • oral
  • forms active metabolite via CYP1A2
  • Fluvoxamine inhibits metabolism
  • SE:
    • dizziness
    • fatigue
    • endrocrine changes
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18
Q

which drug is used in generalized anxiety states

A

Buspirone ( partial 5-HT agonsit, possibly D2-r)

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19
Q

Buspirone mechanism , indication, administration

A
  • ( partial 5-HT agonsit, possibly D2-r)
  • treat : generalized anxiety state
  • oral , forms active metabolite
  • short T1/2
20
Q

buspirone toxicities and interaction

A
  • GI distress
  • tachycardia
  • paresthesia
  • interations with CYP3A4 inducer and inhibitors
21
Q

SSRI (selective serotonin reuptake inhibitors) drugs and mechanism

A
  • Fluoxetine
  • (ES) citalopram
  • Sertraline
  • selective inhibition of 5-HT reuptake (allosterically inhibits transporter)
  • minimal inhibitory effects on NE-transporter, cholinergic, adrenergic receptors
22
Q

SSRI (selective serotonin reuptake inhibitors) characteristics

A
  • oral
  • hepatic metabolism
  • Long T1/2 ( 18-24 hrs) because forms active metabolite
  • Inhibitor of CYp450 enzyme (fluoxetine most potent)
  • treatment response may require up to 4-6 weeks
23
Q

SSRI (selective serotonin reuptake inhibitors) clinical usage

A
  • Major depressive disorders
  • Anxiety disorders ( GAD)
  • OCD
  • PTSD
  • Premenopausal dysphoric disorder (PMDD)
  • panic disorder
  • bulimia

potential OFF-label use of ssri : premature ejaculation

24
Q

SE of SSRI

A
  • Anxiety , agitation
  • sleep disorder
  • bruxism
  • sexual dysfunction (mediated by 5-HT2A r) - Decreased libido, anorgasmia, erectile dys
  • weight gain
  • SIADH
  • withdrawal syndrome : flu-like symptoms, dizziness, anxiety, tremor , palpitation

NOTE: BENZOs may be given as adjunct therapy in first few weeks of ssri treatment to reduce anxiety and agitation

25
Q

Drug interactions ssri

A
  • Inhibition of p450
    • increased level of (due to decreased clearance)
      • TCA ,
      • BENZO
      • warfarin
  • Serotonin syndrome with MAO-A inhibitors , TCA, meperidine
    • muscle rigidity
    • myoclonus
    • hyperthermia
    • CV instability
    • ANS instability

Citalopram is the least frequenctly ass with drug-drug interaction

26
Q

1st gene antipsych. and SE
Also MOA

A

CHF is a chronic old Disease (CHFD)

  • Phenothiazine
    • Chlorpromazine- low potency! Corneal deposits (high dose)
  • thio-xanthenes
    • Flupentixol- wheb you have FLU you PENT IX on ALL
  • Butyrophenones
    • Haloperidol- Neuroleptic malignant Synd. & tardive dyskinesia
    • Droperidol

Promise me there is no Chlor!
Halo! Drop to the Floor

  • All block D2-R >> 5-HT2 r
27
Q

1st gene antipsych. SE

A

Tardive dyskinesia
Hyperprolactinemia
Weight gain (H1 r block)
Autonomic
Thermo

28
Q

Primary indication for antipsych.

A

Schizofrenia

29
Q

1st gene antipsych. are for positive or negative symp?

A

Positive

30
Q

Positive symptoms and which pathway causes it

A
  • increased activity in mesolimbic pathway
    • Thought disorder
    • Delusions
    • hallucination
    • Paranoia/catatonia
    • disorganized speech
  • (New features , no normal/physiologic counter part)
31
Q

negative symptoms of psychosis

A
  • decreased activity of mesocortical pathway
    • Amotivation
    • social withdrawal
    • reduced emotions
    • inability to feel pleasure
  • reduction/removal of normal process
  • Typical agents have NO effect of negative symptoms
32
Q

Effect of 1st gen anti-psychotic based on which tract is inhibited

A
  • blocking Dopamine-receptor in
    • meso-limbic > decreased positive symptoms (delusion, hallucination)
    • meso-cortical > worsening of negative symptoms
      • diminished energy
      • lack of emotion
      • social withdrawal
    • nigrostriatal pathways: extra-pyramidal dysfunction
      • tardive dyskinesia
      • parkinsons like symtpoms
        • muscle rigidity
        • difficulty starting/stoping movement
        • tremors
    • tubulo-infundibal level: increases prolactin
      • galactorrhea
      • gynecomastia
      • sexual dysfunction
33
Q

chlorpromazine effects

A
  • Block D2r>> 5-HT2 r
  • Block alpha, muscurinic, H1-r
  • sedation
  • decreased seizure threshold
34
Q

chlorpromazine indications, administration

A
  • schizophrenia
  • bipolar disorder (manic phase)
  • anti-emesis
  • pre-operative sedation

oral, IV

hepatic metabolism

long T1/2

35
Q

chlorpromazine SE

A
  • extension of alpha & muscurinic receptor blocking actions
  • Extrapyramidal dysfunction
  • Tardive dyskinesia
  • Hyperprolactinemia

Phenothiazine group

36
Q

Flupentixole mechanism, indication, SE

A

Blocks D2r >> 5-HT 2 r

used in schizophrenia

less risk of tardive dyskinesia

Thioxanthene group

37
Q

Haloperidol

doriperidol

mechanism

Administraion

A
  • Block D2r >> 5HT-2 r
  • some alpha block
  • less Muscurinic block
  • less sedation than phenothiazines (chlorpromazine)
  • oral/ I.V
  • hepatic metabolism
38
Q

Haloperidol

doriperidol indication and SE

A
  • schizophrenia
  • bipolar disorder (manic phase)
  • Huntington chorea
  • Tourette syndrome
  • SE: extrapyramidal dysfunction (major)

Neuroleptic malignant syndrome (NMS) (high fever and muscle stiffnes, altered mental status)

and tardive dyskinesia (TD)

39
Q

2nd gene antipsych.

A

Quiet pls! Only Whispering is Appropriate

  • *Quetiapine** and Clozapine. CLOZAP! Quit tipping
  • *Olanzapine**- CLOZ the door with your OLNA
  • *Risperidone**- RiIS got married to mathew PERI and now they are DONE
  • *Aripiprazole**- ARI PIPed to RAZ

**Cariprazine

**Tiapride

40
Q

2nd gene antipsych. dominant MOA

A

5-HT blockade >> D2 r

  • some alpha block ( clozapine, risperidone)
  • M-block ( clozapine, olanzipine)
  • Variable H1-block
41
Q

Antagonism for Benzo’s

A

Flumazenil

مازن is ill with flu

42
Q

Depot injection

A

Injection formulation of a medication which releases slowly over time

43
Q

Antipsychotics antag D2-R MOA

A

D2-R are Gi coupled

  • found in
    • ​caudate
    • putamen
    • nucleus accumbens
    • cerebral cortex
    • hypothalamus

So if we inhibit –> Increased cAMP (Bcs usually if Gi is active the cAMP will decrease)
Increased cAMP causes NF on the Dopamine release

44
Q

D2-R are where?

A

Mesolimbic system
Striatal Frontal System

  • caudate
  • putamen
  • nucleus accumbens
  • cerebral cortex
  • hypothalamus
  • basal ganglia : if d2-r is blocked there > extrapyramidal effects:
    • tremor
    • slurred speech
    • akathisia
    • dystonia
45
Q

2nd gen antipscyotic clinical application and administration

A
  • Schizophrenia (positive & negative symptoms)
  • Bipolar disorder (
    • Olanzipine
    • risperidone
    • quetiapine
    • cariprazine
  • Major depression
    • ​aripiprazole
  • Agitation in alzheimers and parkinsons disease
  • oral, I.V
  • hepatic metabolism
46
Q

2nd gen antipscychotic SE

A
  • Agranulocytosis (clozapine)
  • diabetes & weight gain
    • clozapine
    • olanzapine
    • cariprazine ( D2/D3 antagonist, hungarian development)
  • hyperprolactinemia
    • Risperidone
    • paliperidone
  • QT-prolongation
    • ziprasidone
    • paliperidone
47
Q

Tiapride mechanism and indication

A
  • D2/D3 antagonsit
  • management of alcohol psychosis

Pharmacology FINAL (2nd sem) (37 decks)

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