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Pharmaco > Class 10- geri > Flashcards

Class 10- geri Flashcards

1
Q

ABSORPTION

A

Slower oral absorption
o gastric pH
o intestinal motility
o concentration of proteins responsible for
active transport
Other factors : number of medications, eating
habits, positioning, comorbidities (dysphagia, GERD)
* Clinical impact is not significant

IV routeo Can cause peak effects
IM route: Painful in those with small muscles o Erratic Absorption
Transdermic route o Depending on skin integrity

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2
Q

DISTRIBUTION

A

o lean body mass
o a lot fat body mass (even if small weight!):
FAT SOLUBLE DRUGS: With repeated dosing, drugs can accumulate in fat - distribution volume and half-life
E.g. antidepressants, antipsychotics, benzodiazepines
o total body water small:
WATER-SOLUBLE DRUGS
- distribution volume
- risk of dehydration and adverse effects E.g. lithium
serum albumine: Especially if undernutrition
• unbound concentration of the drug
• E.g. phenytoin, valproate, NSAIDs, warfarin

  • Significant clinical impact
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3
Q

METABOLISM

A

o PHASE I REACTIONS
• Metabolism affected by age
• E.g. accumulation of diazepam and risk of adverse effects
o PHASE II REACTIONS
o Metabolism unaffected with age
• Medications metabolized through glucuronidation are preferred in geriatrics (e.g. oxazepam)

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4
Q

ELIMINATION

A 
o GFR
o drug elimination
o drug half-life
• increase therapeutic and adverse effects of drugs
o decreased dose often needed
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5
Q

PHARMACODYNAMICS

A

Elderly patients have greater psychotropic drug effects than younger patients given the same dose of medication
o greater sensitivity to drugs
o higher concentration at CNS receptors
o Receptor changes with aging
• Cholinergic system : M1 signal transduction, cholinergic activity
• sensivity to anticholinergic effects

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6
Q

DRUG INTERACTIONS ANTIPSYCHOTICS

A 
• Clozapine + benzodiazepines
• Antipsychotics + levodopa
– Good choice  quetiapine, clozapine
• Increased QTc interval
– Especially ziprasidone
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7
Q

Orthostatic hypotension- ANTIPSYCHOTICS

A
  • Less tolerance than adults
  • Risk of falling
  • Choose those who have a low affinity for the alpha 1 receptor
  • E.g. aripiprazole, lurasidone
  • Use a small dose, divide the number of intakes, gradually increase the dose
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8
Q

CHOOSING AN ANTIPSYCHOTIC

A 
1st generation (EPS) vs 2nd / 3rd generation (metabolic effects)
- Long-acting injectables (LAI) can be used
ACCORDING TO COMORBIDITIES
- Diabetes :
✓Best option  aripiprazole
✗Avoid  olanzapine / clozapine
- Glaucoma :
✗Avoid  antipsychotics with anticholinergic effects
- Parkinson’s disease
✓Best options  quetiapine ou clozapine
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9
Q

ANTIDEPRESSANTS SIADH

A

Syndrome of inappropriate ADH secretion

  • Hyponatremia
  • Change in mental status
  • Serious consequences if hyponatremia not treated = coma, death
  • Usually within the first 2 weeks of treatment
  • Serum sodium should be checked before the treatment is treated, and at week 1 and 2 after treatment begins
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10
Q

ANTIDEPRESSANTS Bleeding

A
  • Platelet dysfunction
  • Dose-related effect
  • Increased riks:
  • History of GI bleeding
  • Coagulation disorder
  • NSAIDs
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11
Q

Heart conducting disorders ANTIDEPRESSANTS

A 
Heart conducting disorders
- Especially with tricyclic antidepressants
(risk of arrhythmia)
QTc prolongation
- Maximum dose if > 65 ans :
- Citalopram 20 mg die
- Escitalopram 10 mg die
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12
Q

Choosing an antidepressant

A

✓Best options  SSRI (except paroxetine) or SNRI
- My favourite = sertraline
- Respect maximum doses for citalopram and escitalopram
- Consider ECT
✗Avoid :
✗Paroxetine (anticholinergic effects)
✗Tricyclic antidepressants (anticholinergic effects, cardiac toxicity, drug interactions)
- MAOI (adverse effects, drug interactions)

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13
Q

DRUG INTERACTIONS MOOD STABILIZERS

A

• Several factors can influence the serum
concentration
– Denutrition
– Dehydration
– Interactions with other drugs
– Free (unbound) serum concentration may be relevant for valproate

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14
Q

MOOD STABILIZERS

Choosing a mood stabilizer

A

Bipolar disorder : generally the same as for the adult population

  • Chronic use of a mood stabilizer :
  • Gradual dose reduction is usually required according to liver / kidney function
  • Lithium and valproate
  • Prefer administration once a day at bedtime
  • Aim for the bottom of the therapeutic range (e.g. 0.4 to 0.8 mmol/L for lithium)
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15
Q

BENZODIAZEPINES DRUG INTERACTIONS

A

• Cumulative adverse effects during concurrent use with other psychotropic drugs
• Excessive sedation
• Risk of falling
– Cognitive impairment

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16
Q

Choosing a benzodiazepine

A
  • Always consider other alternatives. If a benzodiazepine MUST be used :
    ✓Best options  benzodiazepines metabolized by glucuronidation
  • Lorazepam, oxazepam, temazepam
    ✗ Other benzodiazepines metabolized by oxidation / long half-life / active metabolites
    ✗Other sedatives / hypnotics to avoid :
    ✗Barbiturates: risk of addiction, abuse
    ✗Over-the-counter antihistamines: e.g. diphenhydramine
  • Non-benzodiazepine receptor agonists (e.g. zopiclone) : more favourable side effects profile but still not recommended according to Beers criteria
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17
Q

PRINCIPLES OF DRUG THERAPY REASSESSMENT IN ELDERY

A
  1. Indication of drugs
  2. Recent modification to pharmacotherapy
  3. Barriers to adherence
  4. Adverse effects
  5. Drug cascade
  6. Drug interactions
  7. Potentially inappropriate drugs
  8. Age-appropriate dosage
  9. Prioritize interventions
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18
Q

INDICATION OF DRUGS

A 
Reason for consultation?
Treatment for every health problem?
Indication for each prescribed drug?
Efficiency?
- Duplication?
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19
Q

RECENT MODIFICATION TO

PHARMACOTHERAPY

A

Timeline of events vs. new health problems

- Appropriate follow-up when adding a drug

20
Q

BARRIERS TO ADHERENCE

A 
MEDICATION MANAGEMENT
- Doset ***
- Help from family / caregivers
- Drugs managed by resource
- More frequent services (e.g. weekly delivery)
KNOWLEDGE OF MEDICATION
- Education to patient / family
- Written information
- Valid references
- Image of different drugs
- List of drugs
DOSING REGIMEN
Reducing the number of tablets
- Facilitate the posology
COGNITIVE/FUNCTIONAL L IMITATIONS
Consider visual/hearing impairment
Dexterity
- Dysphagia
o Alternatives to oral medication :
patch, syrup, crushed tablets, etc.
21
Q

Common side effects in elderly patients

A 
oOrthostatic hypotension
o Posture and balance disorders
o Falls and fractures
o Delirium and cognitive disorders
o Electrolytic disorders
o Heart failure
o Urinary incontinence
o Fatigue, weakness
o Anorexia and weight loss
o Immobilization syndrome
22
Q

BEERS CRITERIA what to avoid

A

Unestablished clinical effectiveness OR other more effective/safe options
Risks > benefits
Anticholinergic properties
- Combination of drugs with an effect on the central nervous system
Avoid anticholinergics, TCAs and bentos

23
Q

AGE-APPROPRIATE DOSAGE

A

Patient weight
Serum creatinine
Patient nutritional status
- Lower doses than adults

24
Q

ALZHEIMER’S DISEASE (AD)

NEUROTRANSMITTERS

A

ACETYLCHOLINE
- Degeneration of cholinergic neeurons
- Loss of choline acetyltransferase (enzyme that makes acetylcholine) and acetylcholinesterase (AChE) activity (enzyme that degrades acetylcholine)
GLUTAMATE
- glutamate in moderate to severe AD
- calcium influx into neurons and speeding up cell death

25
Q

ALZHEIMER’S DISEASE (AD) Avoid

A

medications that can cause cognitive impairment
Anticholinergic or confusion drugs
- Anticholinergics
- Tricyclic antidepressants
- First-generation antihistamines
- Some antipsychotics, opioids, benzodiazepines, narcotics
- Etc.

26
Q

ALZHEIMER’S DISEASE (AD) Pharmacological treatment

A
  1. Acetylcholinesterase inhibitors: Donepezil
    Galantamine, Rivastigmine
  2. Memantine
    • If moderate to severe dementia only
    Drug effectiveness
    - Diminution de la progression de la maladie
    - Aucun effet curatif / aucun renversement des pertes de mémoire
27
Q

DONEPEZIL

A

ARICEPT
REVERSIBLE ACETYLCHOLINESTERASE INHIBITOR
Specific aspects :
Good oral absorption, 100% bioavailability
RDT formulation: rapid dissolution
• Metabolized mainly by CYP2D6 and CYP3A4

28
Q

RIVASTIGMINE

A

EXELON
ACETYLCHOLINESTERASE AND BUTYRYLCHOLINESTERASE INHIBITOR
Specific aspects :
BID
Available by oral administration or patch
• Little metabolized by cytochromes

29
Q

Benefits of RIVASTIGMINE patch

A 
less Fluctuations in absorption and plasma levels
Better tolerance
Easier to ensure a good adherence (?)
Interesting if difficulty swallowing
less s/e on the GI system
30
Q

GALANTAMINE

A 
(REMINYLTM)
REVERSIBLE ACETYLCHOL INESTERASE INHIBITOR AND ALLOSTERIC MODULATION OF NICOTINE RECEPTORS
Specific aspects :
BID or die if ER formulation
• Metabolized by CYP2D6 and CYP3A4
31
Q

CHOLINESTERASE INHIBITORS s/e

A

GI ADVERSE EFFECTS
Especially at the beginning of treatment:
Nausea, vomiting, diarrhea, anorexia and weight loss
Increased risk of gastric bleeding
• Lesser with rivastigmine patch
OTHER ADVERSE EFFECTS
Insomnia and nightmares, Bradycardia, syncope, arrhythmias, Muscle cramps or myalgias
• Skin irritation with rivastigmine patch

32
Q

CHOLINESTERASE INHIBITORS contraindications

A

Heart problem

• Ulcer

33
Q

CHOLINESTERASE INHIBITORS PHARMACOKINETICS DRUG INTERACTIONS

A
  • Donepezil et galantamine
  • Via CYP2D6 and CYP3A4
  • Rivastigmine less at risk of pharmacokinetic interactions
34
Q

CHOLINESTERASE INHIBITORS PHARMACODYNAMIC DRUG INTERACTIONS

A
  • Anticholinergic: antagonism of action
  • Beta blockers /digoxin: bradycardia
  • NSAIDs: increased risk of gastrointestinal effects
35
Q

CHOLINESTERASE INHIBITORS

INTRODUCING TREATMENT

A

Start at the lowest dose

  • Take with food
  • GI adverse effects
  • Administer early in the day
  • insomnia
  • Gradually increase the dose every 4 to 6 weeks if good tolerance
  • Authorization request
  • Renew during treatment to prove that the patient’s condition does not deteriorate too quickly
36
Q

CHOLINESTERASE INHIBITORS

SUBSTITUTION FOR INTOLERANCE

A

Change to another cholinesterase inhibitor:
Stop the first agent
Wait for the full resolution of the adverse reaction
Start the second agent at the usual initial dose
1. Wait at least 4 weeks before a dose increase

37
Q

CHOLINESTERASE INHIBITORS

SUBSTITUTION FOR INEFFICIENCY

A

No downtime required, make the change
the next day:
Start at the usual initial dose
1. Wait at least 2 weeks before a dose increase

38
Q

MEMANTINE

A

NON-COMPETITIVE NMDA RECEPTOR ANTAGONIST
Blocks the effects of abnormally high glutamatergic stimulation while allowing the physiological action of glutamate
• Monotherapy or adjunctive to cholinesterase inhibitor

39
Q

MEMANTINE ADVERSE EFFECTS

A

Generally well tolerated
Dizziness
Headache
- Constipation

40
Q

MEMANTINE DRUG INTERACTIONS

A

Very little
- Increased side effects if associations with
other NMDA receptor ligands (amantadine, DM syrup, ketamine)

41
Q

SCPD ANTIPSYCHOTICS INDICATIONS

A

Failure of non-pharmacological measures
Severe aggression, hallucinations or other behaviours that cause danger to the patient or others
 Risks/benefits were discussed with the patient and his family/caregivers
Atypical antipsychotics preferably: abilify, olanzapine, risperdal, seroquel

42
Q

Risks SCPD ANTIPSYCHOTICS

A

mortality

stroke

43
Q

ANTIPSYCHOTICS

PRINCIPLES OF USE

A

Assess the patient’s risk factors (e.g. history of stroke)
Avoid associations
Start at the lowest possible dose
Use for a short period of time
Monitor for side effects
Reassess regularly: if inadequate response, taper and withdraw. If effective, withdraw attempt in the following months
• Realistic expectations (modest effectiveness)

44
Q

PATHOPHYSIOLOGY delirium

A

CHOLINERGIC DEFICIT• Anticholinergic drugs are often involved in confusing conditions

DOPAMINE EXCESS Dopamine decreases acetylcholine release • Dopaminergic antagonists are sometimes used to treat delirium

45
Q

RISK FACTORS delirium

A 
Head trauma
Drugs: 
* Most common reversible cause
Drugs with anticholinergic effects
Sedatives / hypnotics
Corticosteroids
Narcotics
• Withdrawal (e.g. alcohol, sedatives)
Medical conditions (e.g. electrolytic imbalance, glucose imbalance, infection, dehydration)
Sensory impairments (loss of vision or
hearing
• Environment
46
Q

PHARMACOLOGICAL TREATMENT delirium

A

• Atypical antipsychotics
• Haloperidol
– Few anticholinergic effects, but higher risk of EPS
• Use the smallest dose possible over a short period of time

BENZODIAZEPINES
• To be avoided, as there is an increased risk
of : Sedation, disinhibition, respiratory depression and paradoxical reactions
• To be used if : Delirium secondary to alcohol
withdrawal

Pharmaco (11 decks)

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