pharms Flashcards by Youssef Saifelnasr | Brainscape

Q

Mechanism of Action of benzodiazepines:

A

Bz stimulate specific Bz-receptors — Facilitate GABAA transmission —
Increases CI-influx — Hyperpolarization — Post-Synaptic Inhibition of neurons.

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Q

pharmacological actions of benzodiazepines

A

1- Anxiolytic (Anti-Anxiety):
2- Hypnotic Effects:

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Q

long acting benzodiazepines that have anxiolytic action

A

Diazepam, Chlordiazepoxide and Clorazepate.

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Q

intermediate acting benzodiazepines that have anxiolytic action

A

Oxazepam, Lorazepam and Alprazolam.

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Q

Midazolam!

A

short acting benzodiazepines

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Q

Triazolam!

A

short acting benzodiazepines

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Q

Alprazolam!

A

intermediate acting benzodiazepines

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Q

Clonazepam!

A

intermediate acting benzodiazepines

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Q

Estazolam!

A

intermediate acting benzodiazepines

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Q

Lorazepam!

A

intermediate acting benzodiazepines

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Q

Oxazepam!

A

intermediate acting benzodiazepines

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Q

Temazepam!

A

intermediate acting benzodiazepines

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Q

Chlordiazepoxide!

A

long acting benzodiazepine

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Q

Clorazepate

A

long acting benzodiazepine

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Q

Diazepam

A

long acting benzodiazepine

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Q

Flurazepam

A

long acting benzodiazepine

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Q

Prazepam

A

long acting benzodiazepine

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Q

Quazepam

A

long acting benzodiazepine

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Q

long acting benzodiazepines that have hypnotic effect

A

Flurazepam & Nitrazepam

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Q

Intermediate Acting benzodiazepines that have hypnotic effect

A

Temazepam

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Q

short Acting benzodiazepines that have hypnotic effect

A

Triazolam

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Q

IV Anesthesia benzodiazepine

A

Diazepam
Midazolam

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Q

benzodiazepine that has antidepressant effect

A

Alprazolam

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Q

Therapeutic Uses of benzodiazepines

A

1- Anxiety.
2- Insomnia:
a- Initiate sleep by Triazolam.
b- Maintain sleep by Temazepam or Flurazepam.
3-Preanesthetic medication
4- I.V. Anesthesia
5. Antispasticity
6. Anticonvulsant & Anti-Epileptic:

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Q

Adverse Effects of benzodiazepines

A

1- Dependence — Addiction. Sudden withdrawal — Anxiety & convulsions.
2- Daytime sedation after long acting Bz or Anxiety after short acting Bz.
3- Affect mental. Psycho-motor & Sexual functions.
4- Amnesia (especially Triazolam).
5- Aged patients — mental confusion & hypotension.
6- Additive to Alcohol — Severe CNS Depression.
7- Ataxia.
8-Amenorrhea, decreased Ovulation, decreased Ejaculation & Teratogenic.
9- Increases Appetite — increased Body weight.
10- Allergy.
11-Acute toxicity: Rare unless if used with alcohol — Inhibition of CNS, CVS &
Respiration.

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Q

Treatment of Toxicity of benzodiazepine

A

Flumazenil

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Q

Bz1 receptor agonists

A

Zolpidem, Zaleplon, Zopiclone

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Q

Actions of Barbiturates on C.N.S:

A

1- Sedative action BUT-> Drowsiness.
2- Hypnotic action BUT Abnormal sleep - inhibition of REM:
3- Amnesia.
4- General anesthesia, especially Ultra-short acting barbiturates as Thiopentone.
5- Anticonvulsant as Phenobarbitone
Anti-Epileptic (Phenobarbitone treats Grand Mal & worsens Petit mal epilepsy).

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Q

Mechanism of Action of Barbiturates:

A

Stimulate Specific Barbiturate receptor > GABA-mimetic & facilitate GABA-A transmission - increase CI- influx - Hyperpolarization - Post- synaptic inhibition.

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Q

I.V. Anesthesia barbiturates

A

Thiopentone

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Q

barbiturate treats Grand mal epilepsy, Status epilepticus, febrile convulsions.

A

Phenobarbitone

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Q

Adverse Effects of Barbiturates:

A

Acute Porphyria
Excitation.
Induction of H.M.E. - Tolerance, Cross tolerance, Dependence & Drug Interactions.
Allergy.
Abnormal Sleep - inhibition of R.E.M. - Hang-over & Rebound insomnia.
Amnesia &Automatism.
Acute Poisoning:

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Q

Hypnotic, can be used in extremities of age, especially in children

A

Chloral Hydrate

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Q

Melatonin Agonists:

A

Melatonin, Ramelteon,
Tasimelteon

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Q

Orexin receptor Antagonist:

A

Suvorexant

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Q

Mo

MoA of suvorexant

A

Suvorexant block these OX 1 & 2 receptors to reduce wakefulness and enhance normal sleep.
(orexin is a central peptide neurotransmitter that regulate diurnal rhythm. it high in daylight and low in night to contro wakefullness)

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Q

drug block OX 1 & 2 receptors

A

suvorexant

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Q

Anti-depressant used as anxiolytics

A

Selective serotonin reuptake inhibitors or
Serotonin/norepinephrine reuptake inhibitors (SNRIs)

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Q

drug that its actions are mediated by: serotonin (5-HT14) receptors (a partial agonist), with some affinity for D2 dopamine receptors and 5-HT2a serotonin receptors.

A

buspiron

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Q

buspiron used as

A

anxiolytic

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Q

Treats BOTH Psychic & Somatic (Sympathetic) components of anxiety.

A

Propranolol

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Q

typical anti-psychotic drugs

A

1- Phenothiazines
2- Thioxanthenes
3- butyrophenones

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Q

A

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Q

major drug of Phenothiazines

A

Chlorpromazine
azines

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Q

Pharmacodynamics of phenothiazines on CNS

A

a- Antipsychotic — Blocks Dopamine (D2-receptor)
b- Basal Ganglia — Block D2-receptors — Worsen Parkinsonism.
¢- Hypothalamus:
Hypothermia - Heat loss by cutaneous VD (8 HRC, & VMC &a-Blocker)
increase Appetite & Weight gain.
increase Prolactin.
d- decrease C.T.Z.: Antiemetic in ALL vomiting EXCEPT in motion sickness.

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Q

Pharmacodynamics of phenothiazines on Endocrine

A

a- decrease ACTH
b- decrease FSH &% LH gonadotrophins — Infertility & Amenorrhea in females.
¢- increase Prolactin — Gynecomastia & Galactorrhea

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Q

effect of phenothiazines on receptors

A

potent anti dopamine
potent a blocker
potent antiserotonin
weak anti muscarinic
weak ganglion blocker
weak h1 blocker

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Q

therapeutic uses of phenothiazines

A

1- Psychosis
2- preanesthetic
3- hypothermic
4 hiccough
5- anti-emetic

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Q

tadverse effect of chloropromazine

A

sedation
Acute dystonia
Akathisia
parkinsonism
Neurolept-malignant syndrome (NMS).
Tardive dyskinesia after long use of neuroleptics

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Q

causes Neurolept-malignant syndrome

A

Chlorpromazine

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Q

Pharmacodynamics of phenothiazines on CVS

A

Hypotension & Postural Hypotension —decrease VMC due to a blocker&raquo_space;> direct VD
Tachycardia

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Q

treat Neurolept-malignant syndrome causd by Chlorpromazine

A

IV diazepam or IV dantrolene

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Q

Drug Interactions of Chlorpromazine

A

1- Chlorpromazine Potentiates
a- Sedatives e.g. Alcohol.
b- Hypotensive e.g. V.D. and alpha blockers
¢- Anti-cholinergic e.g. Atropine
d- Muscle relaxants e.g. Curare
2- Chlorpromazine —a-blocker — Reverses pressor effect of Adrenaline.

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Q

Phenothiazine, more potent than chlorpromazine and why?

A

Trifluperazine
more POWERFUL Anti-psychotic &More Extrapyramidal manifestations.

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Q

the Butyrophenones

A

Haloperidol & Droperidol

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Q

used as depot preparation for maintenance treatment in case of non-compliance

A

Haloperidol decanoate

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Q

used in IV. Neurolept Analgesia

A

Droperidol + Fentanyl (Opioid Analgesic)

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Q

treat Neurolept malignant syndrome by

A

IV diazepam or IV dantrolene

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Q

Atypical Anti-Psychotic Drugs that has high incidence of agranulocytosis

A

clozapine

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Q

fluoxetine

A

Selective serotonin re-uptake inhibitors (SSRI)

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Q

imipramine

A

Tricyclic anti-depressants

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Q

venlafaxine

A

Selective norepinephrine serotonin reuptake inhibitors

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Q

trazodone

A

Serotonin (5-HT) receptor modulators

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Q

bupropion

A

unicyclic antidepressants

Q

Pharmacodynamics of Fluoxetine

A

Antidepressant Effect appears after 2-3 WEEKS and lasts for 2-3 WEEKS after stop of SSRI

Q

Therapeutic Uses of fluoxetine

A

Psychic depression
panic disorders
**Obsessive compulsive disorders **
Eating disorders {Bulimia nervosa} » Ineffective in anorexia nervosa
Post-traumatic stress disorder
Premenstrual syndrome — for 2 weeks in Iuteal phase
Premature ejaculation

Q

how to be caution in giving fluoxetine with MAOIs

A

Stop fluoxetine 4-5 weeks before initiating MAOIs

Q

Mechanism of Action of TCA:

A

Inhibit Neuronal Uptakes of Noradrenaline & Serotonin—1 NA, 5-HT Inter-Synaptic.

Q

Actions of Tricyclic Antidepressants

A

1- Antidepressant Effect:
2- SEDATION:
3- Lower Seizure Threshold.
4- Anti-Cholinergic (Anti-Muscarinic = Atropine-Like).
Amitriptyline > Imipramine > Desipramine.
5- Anti-Histaminic (H1-Block) &Ha-Block.
6- Anti-Serotonin.
7- Alpha blocking effect.

Q

members of TCA

A

1-Imipramine
2-Desipramine
3-Clomipramine
4-Amitriptyline
5- Nortriptyline

Q

anti depressant used in nocturnal enuresis

A

Imipramine

Q

treat toxicity of imipramine

A

ICU - Stomach wash + Charcoal.
+ Diazepam — Treats excitement & Seizures.
+ Phenytoin — Treats Seizures & Ventricular arrhythmias.
+ Physostigmine — treats Atropine-like effects.

Q

A

Q

Inhibits reuptake and stimulates release of NA

A

Bupropion

Q

drug interaction of nefazodone

A

Inhibit metabolism of triazolam and simvastatin

Q

from SNRI doesn’t have adverse effect on CNS

A

Milnacipran

Q

Therapeutic Uses of bupropion

A

1- Psychic depression
2-Reduced craving to smoking— As effective as nicotine patches. WHY?
- Mimics effects of nicotine over NA
- Non-competitive blocker of nicotine receptors
- Substitutes for antidepressant effect of nicotine
3-Obesity
4-SSRis-associated sexual side effects

Q

mood stabilizing drugs (antimanic)

A

1- Lithium carbonate
2- Sodium valproate
3- Carbamazepine (oxcarbazepine is ineffective)
4- Lamotrigine

Q

antidepressant used in ceasing smoking

A

bupropion

Q

Herbal Antidepressants:

A

St. John’s Wort

Q

urinary excretion of lithium is increased by

A

Na load
alkalinizer of urine
osmotic diuretics
acetazolamide
loop diuretics

Q

urinary excretion of lithium is increased by

A

hyponatriemia
thiazide diuretics
Spironolactone

Q

Mechanism of Action of lithium carbonate

A

decrease release of noreadrenaline, serotonin & dopamine

Q

Adverse Effects & Toxicity of lithium carbonate

A

Thyroid: Hypothyroidism, Smooth benign enlargement of thyroid gland (Goiter)
a- Initial polydipsia and polyuria » Uncoupling of vasopressin from G proteins&raquo_space; nephrogenic diabetes insipidus.
Teratogenic P Ebstein’s anomaly
overdose needs hemodialysis

Q

Therapeutic Uses of lithium carbonate (mood stabilizer)

A

1- Prophylaxis of Manic-Depressive disorder.
2- Prophylaxis of recurrent endogenous depression.
3- Acute mania but slow onset. So, add antipsychotic drug as haloperidol
4- Management of aggressive & violent behavior in prisoners.

Q

treatment of toxicity of lithium carbonate on kidneys and ADH disorder

A

amiloride

Q

how to deal with over dose of lithium carbonate

A

Hemodialysis

Q

Anti-Parkinsonian Drugs

A

Dopaminergic Drugs
1- Levodopa(L-DOPA) + peripheral dopa decarboxyalse inhibitors Carbidopa
2- COMT-Inhibitors: Tolcapone & Entacapone.
3- MAO-B Inhibitors: Selegiline.
4- Direct Dopamine Agonists: bromocriptine
Anti-Cholinergic Drugs
Benztropine.
Benzhexol
Biperiden

Q

COMT inhibitors

A

Tolcapone
Entacapone
Opicapone

Q

what is mao b inhbitors

A

inhibit enzymers mao b that metabolize dopamine

Q

Bromocriptine used in

A

a- Parkinsonism — Monotherapy or as Add-on to Sinemet.
b- Prolactin — Treat Hyperprolactinemia e.g. Galactorrhea-amenorrhea syndrome.
¢- Suppress lactation. Safer than Estrogen.
d- Acromegaly.

Q

antiviral agent and treats parkinsonism

A

Amantadine

Q

used as an adjunct treatment to L-DOPA and carbidopa to treat the “off” episodes.

A

Istradefylline

Q

Used mainly to treat latrogenic Parkinsonism induced by neuroleptic drugs.

A

Anticholinergic drugs : benzotropine, benzhexol, biperiden

Q

common antiepleptic drug

A

phenytoin

Q

uses of phenytoin

A

Grand Mal Epilepsy & Partial seizures (No Sedation).
2- Status Epilepticus (not first-line).
3-Class-1 Group-B Anti-Arrhythmic Useful in treatment of Ventricular arrhythmia with Heart Block— Drug of Choice in Digitalis-Induced arrhythmia.

Q

causes ginvial hyperplasia

A

phenytoin

Q

carbamzepine uses

A

Grand Mal Epilepsy & Partial seizures
Trigeminal neuralgia
Mood stabilizer

Q

Drug of choice in patients with:
- Mixed Petit mal + Grand mal epilepsy.
- Myoclonic epilepsy.

A

Valproic Acid or Sodium Valproate

Q

First choice:

Absence Seizures = Petit Mal Epilepsy:

A

Ethosuximide

Q

first-line drug of choice for generalized absence seizures (Petit Mal
epilepsy)

A

Ethosuximide

Q

First choice:

Grand Mal Epilepsy & B) Partial seizures:

A

Carbamazepine & lamotrigine & phenytoin

Q

First choice:

Mixed Petit mal + Grand mal epilepsy:

A

Valproate

Q

First choice:

Status Epilepticus treatment:

A

diazepam or lorazepam
phenytoin
fosphenytoin
phenobarbitone

Q

First choice:

Drug-induced Seizures:

A

Benzodiazepines

Q

First choice:

Febrile convulsions in children

A

Valproate,

Q

absorption of morphine

A

SC and IM
in shock&raquo_space; slow diluted IV

Q

what morphine causes to baby during labor

A

Neonatal asphyxia

Q

How to treat Neonatal asphyxia

A

Treat by Naloxone

Q

more active than morphine

A

morphine 6 glucuronide

Q

treat toxicity of morphine

A

stomach wash

Q

w

mechanism of action of morphine

A

1- Inhibit Adenylate cyclase — Decrease CAMP
2- Open K* Channel — Hyperpolarization.
3- Block Ca Channel — Decrease Release of transmitters

Q

effect of morphine on CNS

A

depressant actions:
analgesic of pain
narcosis
cough center
VMC
HRC
hormones ACTH FSH & LH
stimulant actions:
1) euphoria
2) 3 cranial nerve miosis
3) vagal center bradycardia
4)

وجع سناتر هرموات رفلكسات

Q

causes Pin Point Pupil

A

morphine

Q

Morphine-like on GIT —Treat diarrhea with
minimal or No CNS actions.

A

Loperamide & Diphenoxylate

Q

mechanism of action of morphine

A

Effective in all types of pain especially Deep visceral pain.
Inhibits Release of Substance-P & Glutamate in Substantia gelatenosa
inhibit pain transmission
A.N.S inhibit sympathetic and induce parasympathetic
Eye&raquo_space; Miosis&raquo_space; Pin Point Pupil (PPP)
C.V.S.—»Bradycardia & Hypotension
respiratory (Depresses R.C.- depresses cough center- Histamine release» bronchospasm)
spasmogenic
1) smooth muscle
2) GIT&raquo_space; constipation
3) biliary tract
4) urinary tract

Q

Specific Morphine Antagonists

A

Naloxone

Q

Adverse Effects of Morphine

A

1- Interfere with proper diagnosis of Head injury & Acute abdomen.
2- Inhibition of Respiration
3- Pin point pupil (PPP)
4- Nausea & Vomiting
5- Bronchospasm
6- Constipation
7- Retention of urine
8- Neonatal asphyxia
9- ltching
10- Tolerance & cross-tolerance with other Opioids.

Q

imp morphine adverse effects

A

Acute Morphine Poisoning:
Chronic Poisoning» Addiction

Q

Therapeutic Uses of Morphine

A

1- Pain: Analgesic in Severe Visceral Pain
2- Pulmonary Edema due to Acute Left Ventricular Failure
3- Primary Neurogenic shock
4- Preanesthetic medication:

Q

to treat renal and biliary colic by morphine you should add

A

artopine

Q

management of Morphine addiction

A

Hospitalization + Psychotherapy.
Gradual withdrawal of Morphine till the stabilizing dose.
Gradual substitution with Methadone— Similar to Morphine put Less withdrawal manifestations
Gradual withdrawal of Methadone.
Clonidine — Control many withdrawal symptoms.
Acupuncture — Increases Release of endogenous endorphins & enkephalins.
Oral Naltrexone —p-Antagonist — inhibits Euphoria — Dysphoria.

Q

Contraindications of Morphine

A

Head injury
Increased Intra-cranial tension.
Epilepsy
Asthma & chronic obstructive pulmonary disease
Pregnancy & Labor&raquo_space; neonatal asphyxia
Pregnancy & Labor:

Q

use of Papaverine

A

Smooth muscle e.g. Bronchial, Biliary, GIT, Urinary & Uterus —
Useful in Colic.

Q

therapeutic uses of Meperidine

A

1- Severe Visceral pain e.g. Myocardial infarction.
2- Alone in Biliary & Renal colic.
3- Pre-anesthetic medication (Better than Morphine).
4- Obstetric Analgesia: Less inhibition of Fetal R.C.

Q

Therapeutic Uses of codiene

A

Antitussive
Analgesic in Mild & Moderate visceral pain + Aspirin & Paracetamol.

Q

morphine analogue which is Spasmolytic

A

Papaverine

Q

used in Obstetric Analgesia:

A

Meperidine

Q

used in Neurolept- Analgesia

A

Fentanyl + Droperidol

Q

uses of methadone

A

a- Analgesm in Severe visceral pain e.g. Terminal cancer.
b- To substitute Morphine & Heroin during their withdrawal.

Q

used to substitute Morphine & Heroin during their withdrawal.

A

Methadone

Q

moa of tramadol

A

timulate Opiate receptors & decrease Uptake of Noradrenaline & Serotonin.

Q

Treatment of tramadol toxicity:

A

Airway, Breathing, Oxygen, Circulation (ABC), Vasopressors
5-HT3 antagonists as ondansetron
Naloxone will only revert some of the symptoms, while increasing the risk of seizures

Q

uses of mixed agonist antagonist analgesics

A

diagnosis of morhine addiction
2- IF NO Morphine addiction — Kappa (k)-Agonist — Analgesic.
3- IF Morphine Addiction—u-Antagonist — Withdrawal manifestations.

Q

Therapeutic uses of Naltrexone

A

a- Orally to maintain the Opiate-free state of treated addict.
b- Acute Morphine poisoning.
c-Reduce craving to alcohols and cigarette smoking

Q

Mixed Agonist (k) — Antagonist

A

Pentazocine, Buprenorphine, Nalbuphine and Butorphanol

Q

combined with olanzapine (atypical antipsychotic) for the treatment of schizophrenia and acute or maintenance of patients with bipolar

A

Samidorphan (opioid antagonist)

Q

Therapeutic uses of Naloxone

A

a- Acute Morphine poisoning
b- Opioid-induced Neonatal asphyxia—» Mother (IM) or Neonate (Intraumbilical).
c- Diagnosis of Opioid addiction — S.C. — Withdrawal manifestations e.g. Mydriasis

Q

Mechanism of Action of NSAIDs:

A

Inhibit COX&raquo_space; decrease synthesis of prostaglandins (PGs), Prostacyclin (PGl2) &Thromboxane-A2

Q

w

dynamics of salicylates

A

Aspirin produces irreversible inhibition of COX enzymes (1, 2 & 3) by acetylation.
1-C.N.S:
A) Analgesic:
1- Central mechanism&raquo_space; decrease PG&raquo_space; increase Pain threshold especially in Thalamus.
2- Peripheral mechanism&raquo_space; decrease PG&raquo_space; decrease Sensitivity of Nociceptors (Pain receptors) to Histamine, Bradykinin & 5-HT — Anti-inflammatory.
B) Anti-Pyretic:
1- decrease Synthesis of PG induced by IL & Other cytokines — Reset = Readjust Hypothalamic Heat Regulating Center — increase Heat Loss by:
a- Peripheral V.D. - increase Heat loss by radiation.
b- increase Sweating — increase Heat loss by evaporation.
¢- Mobilizes fluids from tissues to plasma.
2- Toxic Dose — Hyperthermia due to Uncoupling of Oxidative-Phosphorylation.
2-Anti-Inflammatory & Anti-Rheumatic:ٌ
ٌٌRespiratory alkalosis
Toxic dose in Children&raquo_space; Metabolic acidosis
May precipitate bronchial asthma
Pain, Ulcer & Bleeding.
Nephropathy

Q

Peripheral acting opioid antagonists

A

Mechanism of analgesic activity
They block enteric opioid receptors, with limited ability to cross BBB
Members
Methylnaltrexone bromide Naloxegol Alvimopan
Therapeutic uses
Opioid-induced constipation in chronic noncancer pain treatment and late-stage advanced disease
Postoperative ileus following bowel resection

Q

a long-acting potent opioid antagonist

A

Nalmefene

Q

Non-Selective COX ~ Inhibitors:

A

Salicylates: Aspirin — Acetylation — Irreversible inhibition of COX enzymes.
Pyrazolones:
Propionic_acid Derivatives: Naproxen, ibuprofen, fenoprofen, flurbiprofen,
Indoles: Indomethacin,
Fenamates:
Phenylacetic Acid Derivatives: Diclofenac.
Oxicams: Piroxicam,

Q

Selective COX-2 Inhibitors (COXIBs)

A

COXIBs Celecoxib, etoricoxib, parecoxib,

Q

Selective COX-3 inhibitors:

A

Paracetamol

Q

Systemic Uses of aspirin

A

1- Anti-pyretic
2- Analgesic
3- Common cold
4- Rheumatic fever (Arthritis)
5- Leukocytosis.
5- Rheumatoid arthritis
6- Chronic gout
7- Antiplatelet

Q

Adverse Effects & Toxicity of Salicylates:

A

1- Acute Toxicity:
Hyperpyrexia, Hyperventilation & Hyperhidrosis — Dehydration.
Hyperacidity , ulcer , bleeding
acid\base imbalance
4- G.1.T. irritation — Nausea, voting, pain, ulceration & bleeding
9- Nephropathy.

Q

causes reyes syndrome

A

aspirin

Q

managmenet of toxicity of aspirin

A

Stomach wash by Sodium bicarbonate.
Alkalization of urine + Forced diuresis

Q

are useful in Aspirin-induced asthma

A

LOX-inhibitors & Cysteinyl LT-1 receptor blocker

Q

uses of indole derivatives

A

closure of patent ductus arteriosus.
Acute gouty arthritis

Q

Indole derivatives

A

indomethacin

Q

from NSAID causes corneal opacity

A

Indomethacin

Q

treatment of closure of patent ductus arteriosus.

A

Indomethacin

Q

advantage of propionic acid derivatives (profen) on aspirin

A

less gastric irritation

Q

Dynamics of Paracetamol

A

1- Inhibit COX-3 in C.N.S.Mainly— Anti-pyretic Analgesic — As potent as Aspirin.
2- Almost No peripheral Action — Almost No Anti-inflammatory & Almost No effect on respiration, C.V.S., Platelet aggregation, Gastric acidity or Uric acid.

Q

managment of toxicity of paracetamol

A

I.V. N-Acetylcysteine (Rich in S-H) + Oral Methionine.

Q

causes opacities of cornea and lens

A

phenothiazine: chlorpromazine