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

A: 25-28 Flashcards

(47 cards)

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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

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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

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

SSRI (selective serotonin reuptake inhibitors) drugs and mechanism

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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

Study These Flashcards
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

Study These Flashcards
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

Study These Flashcards
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
Drug interactions ssri
* Inhibition of p450 * increased level of (due to decreased clearance) * TCA , * BENZO * warfarin * Serotonin syndrome with _MAO-A inhibitors_ , _TCA_, **_meperidin_**e * muscle rigidity * myoclonus * hyperthermia * CV instability * ANS instability Citalopram is the least frequenctly ass with drug-drug interaction
26
1st gene antipsych. and SE Also MOA
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
1st gene antipsych. SE
Tardive dyskinesia Hyperprolactinemia Weight gain (H1 r block) Autonomic Thermo
28
Primary indication for antipsych.
Schizofrenia
29
1st gene antipsych. are for positive or negative symp?
Positive
30
Positive symptoms and which pathway causes it
* increased activity in mesolimbic pathway * Thought disorder * Delusions * hallucination * Paranoia/catatonia * disorganized speech * (New features , no normal/physiologic counter part)
31
negative symptoms of psychosis
* 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
Effect of 1st gen anti-psychotic based on which tract is inhibited
* *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 leve**l: increases prolactin * galactorrhea * gynecomastia * sexual dysfunction
33
chlorpromazine effects
* Block D2r\>\> 5-HT2 r * Block alpha, muscurinic, H1-r * sedation * decreased seizure threshold
34
chlorpromazine indications, administration
* schizophrenia * bipolar disorder (manic phase) * anti-emesis * pre-operative sedation oral, IV hepatic metabolism long T1/2
35
chlorpromazine SE
* extension of alpha & muscurinic receptor blocking actions * Extrapyramidal dysfunction * Tardive dyskinesia * Hyperprolactinemia Phenothiazine group
36
Flupentixole mechanism, indication, SE
Blocks D2r \>\> 5-HT 2 r used in schizophrenia less risk of tardive dyskinesia Thioxanthene group
37
Haloperidol doriperidol mechanism Administraion
* Block D2r \>\> 5HT-2 r * some alpha block * less Muscurinic block * less sedation than phenothiazines (chlorpromazine) * oral/ I.V * hepatic metabolism
38
Haloperidol doriperidol indication and SE
* 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
2nd gene antipsych.
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
2nd gene antipsych. dominant MOA
5-HT blockade \>\> D2 r * some alpha block ( **clozapine, risperidone)** * **M-block ( clozapine, olanzipine)** * **Variable H1-block**
41
Antagonism for Benzo's
Flumazenil مازن is ill with flu
42
Depot injection
Injection formulation of a medication which releases slowly over time
43
Antipsychotics antag D2-R MOA
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
D2-R are where?
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
2nd gen antipscyotic clinical application and administration
* 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
2nd gen antipscychotic SE
* Agranulocytosis (**clozapine**) * diabetes & weight gain * **clozapine** * **olanzapine** * **cariprazine ( D2/D3 antagonist, hungarian development)** * hyperprolactinemia * **Risperidone** * paliperidone * QT-prolongation * ziprasidone * paliperidone
47
Tiapride mechanism and indication
* D2/D3 antagonsit * management of alcohol psychosis

Pharmacology FINAL (2nd sem) (37 decks)

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