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P33 Flashcards

1
Q

Lithium carbonate

A

Mood stabiliser

Bipolar disorder, mania

Use: Lithium is effective in the treatment of acute mania and in the prophylaxis of manic depression.

MoA: not fully understood, but it is thought that it may substitute for sodium or potassium in the central nervous system.

Lithium is toxic, producing dose-dependent and dose-independent side effects.

SE:

  • Diarrhoea, tremor, confusion.
  • Renal toxicity
  • Decreases thyroid function
  • Many drug interactions (particularly diuretics)
  • In OD = convulsions, coma and death

Contraindications:

  • Significant renal impairment
  • Sodium depletion
  • Dehydration
  • Significant cardiovascular disease
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2
Q

Chlorpromazine

A

Typical antipsychotic

Actions: antipsychotic. apathy and inertia. decreased aggression. antiemetics.

MOA: competitive antagonism of dopamine D2 receptors in mesolimbic and cortical pathways.

Use: Schizophrenia. Psychosis. manic phase of bipolar. Tourette’s. Nausea and vomiting. Aggression in children.

Side effects:
Marked sedation
Extrapyramidal symptoms
Galactorrhoea.; Gynaemcomastia. Weight gain.
Contipation. Dry mouth.
Hypotension

Rare: neuroleptic malignant syndrome
Agranulocytosis. hepatotoxicity

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3
Q

Haloperidol

A

Typical antipsychotic

Actions: antipsychotic. apathy. decreased aggression. antiemetic

MOA: competitive antagonism of dopamine D2 receptors. Increased potency when compared with chlorpromazine

Use: Schizophrenia. Psychosis. Mania. Aggressive behaviour. Tourette’s

Side effects:
Marked EPS
Hyperprolactinaemia
Sedative. Hypotensive
Neuroleptic malignant syndrome
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4
Q

Flupentixol

A

Typical antipsychotic

Action: antipsychotic. antidepressant

MOA: competitive antagonism of dopamine D2 receptors.

Use: schizophrenia. psychosis. bipolar disorders.

Side effects: EPS, hyperprolactinaemia, neuroleptic malignant syndrome

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5
Q

Clozapine

A

Atypical antipsychotic

Action: antipsychotic. effective against positive and negative symptoms

MOA: Actions of 5HT2, muscarinic, alpha 1 adrenoceptors, H1 receptors antagonists.

Use: schizophrenia. Very effective, often used in resistant patients.

Side effects:
Little EPS, constipation, agranulocytosis, epileptic seizures, weight gain, hyperglycaemia, hypotension

Rare: neutropaenia, thromboembolism, cardiomyopathy, myocarditis, aspiration pneumonia

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6
Q

Olanzapine

A

Atypical antipsychotic

Action: antipsychotic. effective against positive and negative symptoms

MOA: Actions of 5HT2, muscarinic, alpha 1 adrenoceptors, H1 receptors antagonists.

Use: schizophrenia. Very effective, often used in resistant patients.

Side effects:
Little EPS, constipation, agranulocytosis, epileptic seizures, weight gain, hyperglycaemia, hypotension

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7
Q

Risperidone

A

Atypical antipsychotic

Actions: antipsychotic. effective against positive and negative symptoms

MOA: Potent antagonists of D2 and 5HT2 and alpha 1 adrenoceptors.

Use: Schizophrenia. Psychosis. Mania.

Side effects: EPS (more than other atypicals), insomnia, sedation, hyperprolactinaemia, weight gain, hypotension, sexual dysfunction, anxiety

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8
Q

Quetiapine

A

Atypical antipsychotic

Actions: antipsychotic.

MOA: antagonism of D2 and 5HT2 receptors.

Use: schizophrenia and other psychotic states. Bipolar disorder.

Side effects:
Weight gain. Hyperprolactinaemia
Minor EPS.
Constipation. Dry mouth. 
Sedation. postural hypotension. 
Rare: neuroleptic malignant syndrome
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9
Q

Sulpiride

A

Atypical antipsychotic

Actions: antipsychotic.

MOA: Dopamine D2 and D3 antagonism. preferential action on dopamine autoreceptors - less EPS.

Use: schizophrenia

Side effects: hyperprolactinaemia. insomnia. anxiety. weight gain. constipation. dry mouth

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10
Q

Amisulpiride

A

Atypical antipsychotic

Actions: antipsychotic.

MOA: Dopamine D2 and D3 antagonism. preferential action on dopamine autoreceptors - less EPS.

Use: schizophrenia

Side effects: hyperprolactinaemia. insomnia. anxiety. weight gain. constipation. dry mouth

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11
Q

Aripiprazole

A

Actions: antipsychotic

MOA: Modifications of dopaminergic transmission. Strongly D2 with partial agonist activity.

Use: schizophrenia. psychosis. manic phase of bipolar

Side effects: fewer side effects than other antipsychotics.
Less weight gain.
Some hypotension and nausea and vomiting.

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12
Q

Lithium

A

Actions: mood stabiliser

MOA: not well understood. Theory that lithium interferes with membrane ion transport including neurotransmitter uptake

Use: bipolar. mania. effects develop over 3-4 weeks

Side effects:

  • Diarrhoea, tremor, confusion.
  • Renal toxicity
  • Decreases thyroid function
  • Many drug interactions (particularly diuretics)
  • In OD = convulsions, coma and death
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13
Q

Carbamazepine

A

Action: antiepileptic. Relieves neuropathic pain. Mood stabiliser

MOA: Blocks Na+ channels to inhibit action potential initiation and propagation. use-dependence of block means that action is preferential on rapid fire neurons

Use: partial and generalised seizures. Not absence seizures. Neuropathic pain. Bipolar disorder

Side effects: drowsiness, headache, mental disorientation, motor disturbances
Rare but serious: agranulocytosis, liver damage, aplastic anaemia
Teratogenic
p450 interaction

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14
Q

Sodium valproate

A

Actions: anticonvulsant, mood stabiliser

MOA: block of Na channels in inhibit action potential initiation and propagation. Inhibition of GABA transaminase to decrease GABA breakdown

Use: epilepsy. manic phase of bipolar, migraine

Side effects: nausea and vomiting. tremor. weight gain. reproductive dysfunction. hepatic and pancreatic toxicity
Teratogenic

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15
Q

Sertraline
Citalopram
Fluoxetine
Paroxetine

A

SSRI - Selective serotonin reuptake inhibitor

Action: antidepressant

MOA: Inhibits the reuptake of 5HT3 into neurons

Use: depression, anxiety

Side effects:

  • Anxiety,
  • Insomnia,
  • Nausea,
  • Diarrhoea,
  • Headache,
  • Sexual dysfunction
  • Increased risk of suicide in younger patients
  • Causes hyponatraemia in the elderly
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16
Q

Duloxetine

Venlafaxine

A

Serotonin-noradrenaline reuptake inhibitors (SNRI)

Actions: antidepressant

MOA: inhibits the reuptake of 5HT and NA into neurons, increasing transmitter action

Use:

  • Major depression
  • Anxiety disorders (panic, GAD, OCD, agoraphobia)
  • Attention-deficit hyperactivity disorder
  • Chronic neuropathic pain
  • Fibromyalgia syndrome (FMS)”

Side effects:

  • Nausea,
  • Headache,
  • Sleep disturbance,
  • Sexual dysfunction
  • Cardiac dysrhythmia, seizure and CNS depression with OD
  • Takes a few weeks to see effects
  • Increase risk of suicide in younger people
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17
Q

Amitriptyline
Imipramine
Lofepramine
Clomipramine

A

TRICYCLIC ANTIDEPRESSANT

Actions: antidepressant, neuropathic pain

MOA: Inhibits reuptake of NA and 5HT3 into neurons, increasing transmitter actions

Use: depression, panic disorder, neuropathic pain. enuresis

Side effects: sedation, blurred vision, dry mouth, constipation, urinary retention

  • Overdose potentially fatal due to cardiac dysrhythmia, severe hypotension, seizure and CNS depression
  • Increased risk of suicide in younger patients
  • Clinical effects not seen for a few weeks
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18
Q

Mirtazapine

A

Presynaptic a2-adrenoceptor blocks

“Presynaptic alpha2-adrenoreceptor antagonist which increases central noradrenergic and serotonergic neurotransmission

Dual mode of action:

  • Noradrenergic and specific serotonergic antidepressant (NaSSA)
  • That acts by antagonizing the adrenergic alpha2-autoreceptors and alpha2-heteroreceptors as well as by blocking 5-HT2 and 5-HT3 receptors

Use: major depression

SE:

  • Anxiety
  • Increased appetite/weight
  • Arthralgia, myalgia
  • Confusion
  • GI symptoms
  • Dizziness, drowsiness, insomnia
  • Dry mouth
  • Headache (on discontinuation)
  • Postural hypotension
19
Q

Phenelzine

A

MOAIs - monamine oxidase inhibitor

Actions: antidepressant

MOA: Irreversibly binds to A and B forms of monoamine oxidase.
MAO-A acts on NA and 5HT
MAO-B acts on dopamine
Inhibiting MAO increases transmitter at nerve endings

Use: atypical depression. social phobia

Side effects: postural hypotension, headache, insomnia, sexual dysfunction
Dry mouth, urinary retention

  • OD = convulsions
  • Increased risk of suicide in young people
  • Dietary TYRAMINE causes hypertensive crisis (Cheese)
  • Antidepressant effect due to MAO-A inhibition
20
Q

Moclobemine

A

MOAIs - monamine oxidase inhibitor (A only)

Actions: antidepressant

MOA: Irreversibly binds to A forms of monoamine oxidase.
MAO-A acts on NA and 5HT
Inhibiting MAO increases transmitter at nerve endings

Use: atypical depression. social phobia

Side effects: postural hypotension, headache, insomnia, sexual dysfunction
Dry mouth, urinary retention

  • OD = convulsions
  • Increased risk of suicide in young people
  • Dietary TYRAMINE causes hypertensive crisis (Cheese)
  • Antidepressant effect due to MAO-A inhibition
21
Q

Isocarboazid

A

MOAIs - monamine oxidase inhibitor

Actions: antidepressant

MOA: Irreversibly binds to A and B forms of monoamine oxidase.
MAO-A acts on NA and 5HT
MAO-B acts on dopamine
Inhibiting MAO increases transmitter at nerve endings

Use: atypical depression. social phobia

Side effects: postural hypotension, headache, insomnia, sexual dysfunction
Dry mouth, urinary retention

  • OD = convulsions
  • Increased risk of suicide in young people
  • Dietary TYRAMINE causes hypertensive crisis (Cheese)
  • Antidepressant effect due to MAO-A inhibition
22
Q

Bupropion

A

DOPAMINE REUPTAKE INHIBITOR

Actions: atypical antidepressant, used in smoking cessation

MOA: inhibits neuronal dopamine reuptake with a lesser effect on NA. Antagonist at nicotinic receptors.

Use: alone or in combination with SSRIs in depression

Side effects: agitation, tremor, dry mouth, nausea, insomnia, skin rashes

Seizures can occur with large doses

23
Q

Non-pharmacological treatment for bipolar disorder?

A

In bipolar disorder, as in unipolar major depression, severe symptoms in the current mood episode compel the use of electroconvulsive therapy (ECT).

Treating bipolar patients with ECT is consistent with numerous practice guidelines.

24
Q

Adverse Drug Reaction (ADR)

A

“An unwanted or harmful reaction experienced following the administration of a drug or combination of drugs under normal conditions of use and suspected to be related to the drug”

Excludes:

  • Therapeutic failures
  • Overdose
  • Drug abuse
  • Non-compliance
  • Medication errors
25
Q

Adverse Drug Event

A

Untoward occurrence after exposure to a drug that is not necessarily caused by the drug

26
Q

Adverse drug reaction vs Adverse drug event?

A

Adverse drug event

  • Patient having a road traffic accident while on a specific medication
  • Untoward occurrence after exposure to a drug that is not necessarily caused by the drug

Adverse drug reaction

  • Patient experiencing anaphylaxis shortly after taking a drug
  • An unwanted or harmful reaction experienced following the administration of a drug or combination of drugs under normal conditions of use and suspected to be related to the drug
27
Q

Adverse drug reaction classification

A

Type A reactions (augmented):

  • Common, 80% of all reactions
  • Are predictable from the known pharmacology of a drug
  • Exaggerated response to pharmacological action
  • Usually dose dependent
  • High incidence (morbidity), low mortality.

Type B reactions:
- Idiosyncratic, bizarre or novel responses that cannot be predicted from the known pharmacology of a drug and are associated with low morbidity and high mortality.

Not all ADRs fit into type A and type B categories; therefore, additional categories have been developed.

Type C (continuing),

Type D (delayed use)

28
Q

These are examples of that type of drug reaction?

  1. Sedation with antihistamines:
    - Blockade of central histaminergic receptor
    - Action on serotonin receptors
  2. Constipation with opioids
    - Stimulation of mu receptors in GIT
  3. Gastric ulcers with NSAIDs
    - Inhibition of prostaglandins which protect stomach
A

Type A adverse drug reaction

29
Q

Drug induced parkinsonism

A
  • Drugs that block the action of dopamine = dopamine antagonists
  • Atypical antipsychotics have less extrapyramidal symptoms
  • Clozapine, olanzapine, risperidone
  • Less affinity for D2 receptors
30
Q

Metoclopramide

A

D2 receptor antagonist.

Indications:

  • Migraine headache treatment
  • Prevent N+V
  • Increase stomach emptying
  • GORD

SE:

  • Fatigue
  • Diarrhoea
  • Restlessness

More serious side effects include:

  • Movement disorder like tardive dyskinesia
  • Neuroleptic malignant syndrome
  • Depression

Causes hyperprolactinemia due to inhibitory effect on prolactin leading to:
- Galactorrhoea, amenorrhoea, breast tenderness

31
Q

First gen antipsychotics

typical

A 
Haloperidol
Chlorpromazine
Fluphenazine
Flupentixol
Sulpiride
Loxapine

SE:
- Extrapyramidal:
> Akathisia (severe restlessness)
> Tardive dyskinesia (involuntary choreoathetoid movements, most common is chewing and pouting of jaw)
> Acute dystonia (e.g. torticollis, oculogyric crisis)
> Dystonia (involuntary muscular contraction)
> Pseudoparkinsonism

  • Hyperprolactinemia
  • Decreased seizure threshold
  • Postural hypotension
  • Sedation
  • Weight gain
  • Prolonged QT interval (particularly haloperidol)
  • Antimuscarinic
32
Q

Second gen antipsychotics

atypical

A 
Risperidone
Paliperidone 
Clozapine
Olanzapine
Quetiapine
Aripiprazole
Amisulpride
SE:
- Metabolic syndrome:
> Weight gain
> Cholesterol abnormalities
> DM II + obesity
  • Reduced seizure threshold (greater with atypicals)
  • Extrapyramidal (akathisia, dyskinesia, dystonia)
  • Salivation
  • Myocarditis
  • Agranulocytosis, neutropenia [clozapine]
33
Q 
Ibuprofen
Naproxen
Diclofenac
Aspirin
Indomethacin
A

Non-selective NSAIDs (COX inhibitors)

The COX-1 enzyme is constitutive and produces prostaglandins associated with GI cytoprotection. The inhibition of these prostaglandins by traditional NSAIDs increases the susceptibility of the GI tract to risk for damage from gastric acid, pepsin, and bile. COX-1 also is associated with prostaglandin production related to the regulation of platelet function (primarily aggregation) and renal function.

The COX-2 enzyme generally is considered to be inducible. It produces prostaglandin secondary to proinflammatory mediators such as cytokines as a response to pain, fever, and inflammation.

SE:

  • Heartburn
  • Dyspepsia
  • Ulceration
  • Bleeding
  • Perforation
34
Q

List penicillins used in combination with a beta-lactamase inhibitor or contain a beta lactam ring

A

Beta-lactamase inhibitor combo: (tazocin & co-amoxiclav)

Contain a beta lactam ring (imipenem & meropenem, carbopenem antimicrobial agents)

35
Q

Naproxen + ramipril?

NSAID + ACEi

A

Combinations of drugs may increase the risk of acute kidney injury, as each has the potential to affect kidney function through different mechanisms.

Angiotensin converting enzyme inhibitors/angiotensin receptor blockers cause a haemodynamic reduction in glomerular filtration rate due to efferent arteriolar vasodilation, and NSAIDs cause inhibition of prostacyclin synthesis leading to renal afferent arteriolar vasoconstriction.

36
Q

Cytochrome P450 3A4 is responsible for metabolism of:

  • Calcium channel blockers
  • Benzodiazepines
  • HIV protease inhibitors
  • HMG-CoA-reductase inhibitors
  • Ciclosporin
  • Non-sedating antihistamines

And is present in GIT and liver.

What are it’s inhibitors and inducers?

A

Inhibitors

  • Fluconazole
  • Clarithromycin
  • Erythromycin
  • Grapefruit juice
  • Ritonavir

Inducers

  • Carbamazepine
  • Rifampicin
  • Rifabutin
  • St. John’s wort
Enzyme induction
leads to:
- Tolerance or decreased effectiveness
- Increased doses
- Increased metabolism and excretion
- Slow development -days to weeks
Enzyme inhibition
 leads to:
- Sensitivity
- Decreased doses
- Drug accumulation
- Rapid development -days
37
Q

What are the implications of being a CYP2D6 ultra-rapid metaboliser?

A

CYP2D6 is highly polymorphic, with over 90 known allelic variants.

Codeine is a prodrug and its analgesic properties are not manifest until it is metabolized by CYP2D6, primarily to morphine and and codeine-6-glucuronide. Subjects who are ultra-rapid metabolizers based upon CYP2D6 genotype have higher than expected morphine levels (an initial “overdose”), with more side effects and a shorter than expected duration of pain control.

38
Q

List opiates which are potentially affected by the CPY2D6 polymorphism.

A

Codeine
Hydrocodone
Oxycodone
Tramadol

39
Q

Azathioprine

A

Antiproliferative immunosuppressant

Action: decreases clonal proliferation of T and B cells during induction phase of immune response

MOA: interferes with purine synthesis. cytotoxic on dividing cells

Use: UC and Crohn’s. prevent organ rejection. chronic autoimmune disease, rheumatoid arthritis, granulomatosis with polyangiitis.

SE: myelotoxicity. GI disturbance. hypersensitivity reactions

NOTE: monitor blood for myelosuppression

40
Q

Pharmacogenomics vs pharmacogenetics

A

Pharmacogenetics focuses on single drug-gene interactions.

Pharmacogenomics encompasses a more genome-wide association approach, incorporating genomics and epigenetics while dealing with the effects of multiple genes on drug response

41
Q

Which electrolyte abnormality could an ACEi and spironolactone cause?

A

Hyperkalaemia

42
Q

The four major causes of hyperkalemia due to reduced urinary potassium secretion are?

A

●Reduced aldosterone secretion

●Reduced response to aldosterone (aldosterone resistance)

●Reduced distal sodium and water delivery as occurs in effective arterial blood volume depletion

●Acute and chronic kidney disease in which one or more of the above factors are present

43
Q

How is GFR measured?

A

Although GFR cannot be measured directly, the best method for determining GFR is measurement of the urinary clearance of an ideal filtration marker.

The gold standard of exogenous filtration markers is inulin. Inulin is a physiologically inert substance that is freely filtered at the glomerulus, and is neither secreted, reabsorbed, synthesized, nor metabolized by the kidney. Thus, the amount of inulin filtered at the glomerulus is equal to the amount excreted in the urine, which can be measured. Inulin, however, is in short supply, expensive, and difficult to assay. Furthermore, the classic protocol for measuring inulin clearance requires a continuous intravenous infusion, multiple blood samples, and bladder catheterization.

The most common methods utilised to estimate the GFR are: measurement of the creatinine clearance; and estimation equations based upon serum creatinine such as the Cockcroft-Gault equation, the Modification of Diet in Renal Disease (MDRD) study equations, and the Chronic Kidney Disease Epidemiology Collaboration (CKD-EPI) equation.

44
Q

Oral iron:

  • Ferrous sulfate
  • Ferrous fumarate
  • Ferrous gluconate

Parenteral iron:

  • Iron dextran
  • Iron sucrose
  • Ferric carboxymaltose
  • Iron isomaltoside 1000
A

Parenteral iron is generally reserved for use when oral therapy is unsuccessful because the patient cannot tolerate oral iron, or does not take it reliably, or if there is continuing blood loss, or in malabsorption.

Dietary iron is absorbed from the duodenum and upper jejunum.

Haem dietary sources (fish, poultry, and meat) have a higher bioavailability than do non-haem (vegetable) sources (30 versus 10 percent).

= Ascorbic acid (Vitamin C) enhances the absorption of non-animal sources of iron.
= Phosphates, and phytates inhibit iron absorption.

Absorption of ferric iron is facilitated by several factors:

  • Gastric acid, which increases its solubility
  • Conversion to ferrous iron by ferric reductase on the brush border of enterocytes, which is enhanced by dietary reducing agents such as ascorbic acid (vit C), fructose and some amino acids,
  • Intestinal absorption mediated by the divalent metal transporter (DMT-1), mainly in the duodenum.

Expression of DMT-1 is increased in iron deficiency and in hereditary haemochromatosis.

Within enterocytes, iron is oxidized to the ferric state and transported to the circulation by the protein ferroportin.

In the blood, ferric iron is bound to the globulin transferrin and transported to the bone marrow and iron stores.

Cellular iron uptake occurs via transferrin receptors, and in most cells iron is stored as ferritin (a complex of iron with the apoferritin protein).

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