Immunomodulators and Antineoplastics Flashcards
What class of drug is Prednisolone (Panafcortelone, Predsolone, Solone)?
Glucocorticoid
What class of drug is Promethazine (Phenergan)?
Sedating antihistamine
What class of drug is Cetirizine (Zyrtec)?
Less sedating antihistamine
What class of drug is Loratidine (Claratyne) ?
Less sedating antihistamine
What class of drug is Methotrexate (Methoblastin)?
Folic acid antagonist
What class of drug is Anakinra (Kineret)?
IL-1 receptor antagonist
What class of drug is Cyproterone acetate (Procur, Androcur)?
Anti-androgen
What class of drug is Dexamethasone (Dexmethsone)?
Synthetic corticosteroid
What class of drug is Leuprorelin (Eligard, Lucrin)?
GnRH agonist
What class of drug is Tamoxifen (Nolvadex)?
Selective oestrogen receptor modulator
What class of drug is Letrozole (Femara)?
Aromatase inhibitor
What class of drug is Hydrocortisone (Hysone, Sigmacort)?
Synthetic corticosteroid
What is the mechanism of action of Prednisolone (Panafcortelone, Predsolone, Solone)?
Corticosteroids regulate gene expression, which results in:
- Glucocorticoid effects, e.g. gluconeogenesis, proteolysis, lipolysis, suppression of inflammation and immune responses
- Mineralocorticoid effects, e.g. hypertension, sodium and water retention, potassium loss
What is the mechanism of action of Promethazine (Phenergan)?
Reduce the effects of histamine by binding to the H1 receptor and stabilising it in an inactive form
They also have anticholinergic activity and some have alpha-blocking activity
What is the mechanism of action of Cetirizine (Zyrtec)?
Reduce the effects of histamine by binding to the H1 receptor and stabilising it in an inactive form
What is the mechanism of action of Loratidine (Claratyne) ?
Reduce the effects of histamine by binding to the H1 receptor and stabilising it in an inactive form
What is the mechanism of action of Methotrexate (Methoblastin)?
Inhibits DNA synthesis and cell replication by competitively inhibiting the conversion of folic acid to folinic acid as it resembles the structure of folic acid
It has cytotoxic, immunosuppressive and anti-inflammatory action
What is the mechanism of action of Anakinra (Kineret)?
Recombinant form of human interleukin-1 (IL-1) receptor antagonist; it neutralises the activity of IL-1, which is involved in acute inflammatory response
What is the mechanism of action of Cyproterone acetate (Procur, Androcur)?
Competitively inhibits the binding of androgen at androgen receptors
Cyproterone (a steroidal anti-androgen) also has progestogenic effects that result in decreased production of testosterone
What is the mechanism of action of Dexamethasone (Dexmethsone)?
Regulates gene expression, which results in mainly glucocorticoid effects, but also some mineralocorticoid effects
Acts as an anti-inflammatory and immunosuppressant, mimicking the effect of cortisol but with 20 to 30 times the potency. It is 4 to 5 times more potent than prednisone
With steroid treatment, it is critical to progressively reduce dosage rather than stop administration abruptly. This is because the adrenal glands significantly reduce steroid production when levels are high (due to treatment) and it takes some weeks to recover from induced adrenal insufficiency
What is the mechanism of action of Leuprorelin (Eligard, Lucrin)?
GnRH initially stimulates synthesis of FSH and LH, transiently increasing serum testosterone in males or serum oestrogen in females
Continuous administration of GnRH agonists inhibits gonadotrophin production, suppressing ovarian and testicular steroidogenesis and inhibiting the growth of certain hormone-dependent tumours
What is the mechanism of action of Tamoxifen (Nolvadex)?
Competes with oestrogen for receptor sites in breast tissue (anti-oestrogenic effect) inhibiting tumour growth
Also have oestrogen agonist activity on endometrium, bone and lipids
Suppression of other growth factors and cytokines may occur
What is the mechanism of action of Letrozole (Femara)?
Aromatase enzymes (in fat, liver, muscle and breast tissue of postmenopausal women) convert circulating androstenedione and testosterone to oestriol and oestradiol
Aromatase inhibitors reduce tissue oestrogen concentration
What is the mechanism of action of Hydrocortisone (Hysone, Sigmacort)?
Regulates gene expression, which results in both glucocorticoid and mineralocorticoid effects
In the kidney, cortisol is a potent agonist of the mineralocorticoid receptor. However, these mineralocorticoid receptors are ‘shielded’ from cortisol by the action of 11β-HSD 2, which converts active cortisol into inactive cortisone. This mechanism ensures that, at physiologic levels, cortisol does not exert mineralocorticoid effects
At high concentrations, however, cortisol can overwhelm the capacity of 11β-HSD 2, leading to stimulation of renal mineralocorticoid receptors
What are the side effects of Prednisolone (Panafcortelone, Predsolone, Solone)?
- Adrenal suppression
- Increases susceptibility to infection
- Sodium and water retention
- Oedema
- Hypertension
- Hypokalaemia
- Hyperglycaemia
- Dyslipidaemia
- Osteoporosis
- Increased appetite
- Dyspepsia
- Delayed wound healing
- Bruising
- Acne
- Facial flushing
- Hirsutism
- Growth retardation in children
- Myopathy
- Muscle weakness
- Fat redistribution (cushingoid appearance)
- Weight gain
- Amenorrhoea
- Psychiatric effects
What are the side effects of Promethazine (Phenergan)?
- Sedation
- Psychomotor impairment
- Dizziness
- Confusion
- Headache
- Blurred vision
- Mydriasis
- Dry eyes
- Constipation
- Dry mouth
- Urinary retention
- Nausea
- Vomiting
- Diarrhoea
- Hypotension
What are the side effects of Cetirizine (Zyrtec)?
- Drowsiness
- Fatigue
- Headache
- Nausea
- Dry mouth
What are the side effects of Loratidine (Claratyne) ?
- Drowsiness
- Fatigue
- Headache
- Nausea
- Dry mouth
What are the side effects of Methotrexate (Methoblastin)?
- Drowsiness
- Fatigue
- Headache
- Nausea
- Dry mouth
What are the side effects of Anakinra (Kineret)?
- Injection site reactions
- Headache
- Serious infections
- Neutropenia
- Allergy
What are the side effects of Cyproterone acetate (Procur, Androcur)?
- Cognitive changes
- Oedema
- Inhibition of spermatogenesis
- Reduced ejaculate volume
- Allergic reactions
- Reduced adrenal function
- Depression
- Shortness of breath
- Thromboembolism
- Anaemia
- Tachycardia
- Osteoporosis
- Reduced libido
What are the side effects of Dexamethasone (Dexmethsone)?
- Adrenal suppression
- Increases susceptibility to infection
- Sodium and water retention
- Oedema
- Hypertension
- Hypokalaemia
- Hyperglycaemia
- Dyslipidaemia
- Osteoporosis
- Increased appetite
- Dyspepsia
- Delayed wound healing
- Bruising
- Acne
- Facial flushing
- Hirsutism
- Growth retardation in children
- Myopathy
- Muscle weakness
- Fat redistribution (cushingoid appearance)
- Weight gain
- Amenorrhoea
- Psychiatric effects
What are the side effects of Leuprorelin (Eligard, Lucrin)?
- Decreased BMD
- Altered glucose tolerance
- Diabetes
- Anaemia
- Increased body fat
- Weight gain
- Muscle atrophy
- Hair changes (loss of body hair)
- Cardiovascular disease
- Tumour flare
What are the side effects of Tamoxifen (Nolvadex)?
- Leg cramps
- Alopecia
- Hot flushes
- Sweating
- Vaginal discharge
- Nausea
- Oedema
- Increase in hepatic enzymes and bilirubin
- Uterine polyps
- Impotence or loss of libido
- Endometrial cancer
- Non-alcoholic steatohepatitis
What are the side effects of Letrozole (Femara)?
- Hot flushes
- Vaginal dryness
- Weakness
- Headache
- Nausea
- Vomiting
- Diarrhoea
- Myalgia
- Arthralgia
- Reduced BMD (bone mineral density)
- Fractures alopecia
- Rash
- Peripheral oedema
- Carpal tunnel syndrome
What are the side effects of Hydrocortisone (Hysone, Sigmacort)?
- Adrenal suppression
- Increases susceptibility to infection
- Sodium and water retention
- Oedema
- Hypertension
- Hypokalaemia
- Hyperglycaemia
- Dyslipidaemia
- Osteoporosis
- Increased appetite
- Dyspepsia
- Delayed wound healing
- Bruising
- Acne
- Facial flushing
- Hirsutism
- Growth retardation in children
- Myopathy
- Muscle weakness
- Fat redistribution (cushingoid appearance)
- Weight gain
- Amenorrhoea
- Psychiatric effects
What are the indications for use of Prednisolone (Panafcortelone, Predsolone, Solone)?
Administration: oral tablet, liquid
- Acute asthma
- Autoimmune or inflammatory disease
- Acute gout
- Croup
- Multiple myeloma
- Lymphoma
- Some leukaemias
Contraindications:
History of recurrent infections
Latent TB
PUD
Diabetes (worsens control)
Hypertension, heart failure
Psychiatric disorders
Glaucoma
Osteoporosis
Myasthenia gravis
What are the indications for use of Promethazine (Phenergan)?
Administration: IM, oral tablet, oral liquid
- Allergic conditions (e.g. rhinitis, urticaria)
- Itch
- Nausea and vomiting
- Motion sickness
- Sedation (short term)
Contraindications:
PKU
Epilepsy
Respiratory depression
Parkinson’s disease
Elderly patients
Children
What are the indications for use of Cetirizine (Zyrtec)?
Administration: oral tablet, oral liquid
- Allergic rhinitis
- Chronic urticaria
Most likely of the less sedating antihistamines to cause sedation
What are the indications for use of Loratidine (Claratyne) ?
Administration: oral tablet, oral liquid
- Allergic rhinitis
- Chronic urticaria
What are the indications for use of Methotrexate (Methoblastin)?
Administration: oral tablet, IM, SC
- Various cancers
- Psoriasis
- Rheumatoid arthritis
- Crohn’s disease
- Ectopic pregnancy
- Polymyositis, dermatomyositis
What are the indications for use of Anakinra (Kineret)?
Administration: SC injection
- Rheumatoid arthritis (in conjunction with methotrexate)
- Gout
- Destructive osteoarthritis
- Type II DM
Contraindications:
Untreated or serious infection
May reactivate hepatitis B and latent TB (begin TB treatment before starting anakinra)
Surgery
Response to treatment usually occurs within 2 weeks with maximum benefit by 12 weeks. Measure complete blood count before treatment.
What are the indications for use of Cyproterone acetate (Procur, Androcur)?
Administration: oral tablet
- Metastatic prostate cancer
- Moderately severe-to-severe signs of androgenisation in women (hirsutism, alopecia, acne, seborrhoea)
- Prevention of GnRH agonist-associated initial tumour flare
- Hot flushes associated with orchiectomy or HbRH agonist
- Reduction of sexual drive in men
Contraindications:
Meningioma
Thromboembolic disease, sickle cell anaemia, diabetes with vascular disease
Severe chronic depression
Diabetes
Pregnancy
What are the indications for use of Dexamethasone (Dexmethsone)?
Administration: oral tablet, liquid, intra-articular injection
- Cerebral oedema due to malignancy
- Croup
- Autoimmune conditions, such as rheumatoid arthritis
- Allergic anaphylactic shock
- Bacterial meningitis
- To counteract side-effects of anti-tumour treatment
- Promote maturation of foetal lungs in women at risk of delivering prematurely
- High altitude sickness
- Adrenal insufficiency and Addison’s disease
Contraindications:
History of recurrent infections
Latent TB
PUD
Diabetes (worsens control)
Hypertension, heart failure
Psychiatric disorders
Glaucoma
Osteoporosis
Myasthenia gravis
What are the indications for use of Leuprorelin (Eligard, Lucrin)?
Administration: SC, IM injection
- Locally advanced or metastatic prostate cancer
- Precocious puberty
- Pituitary down regulation to prepare for controlled ovarian stimulation
Contraindications:
Low bone mineral density
Vertebral metastases
What are the indications for use of Tamoxifen (Nolvadex)?
Administration: oral tablet
- Hormone receptor-positive advanced breast cancer
- Hormone receptor-positive early breast cancer (adjuvant)
- Primary prevention of breast cancer in high-risk women
Contraindications:
Pre-existing endometrial hyperplasia
History of thromboembolic disease
Chemotherapy
Pregnancy
What are the indications for use of Letrozole (Femara)?
Administration: oral tablet
- Hormone receptor-positive early breast cancer in postmenopausal women (initial or extended adjuvant therapy)
- Hormone receptor-positive advanced breast cancer in postmenopausal women (first-line treatment or after failure of tamoxifen)
Contraindications:
Pre- or perimenopause
Low BMD
Pregnancy
What are the indications for use of Hydrocortisone (Hysone, Sigmacort)?
Administration: oral tablet, intra-articular injection
- Adrenal insufficiency (e.g. Addison’s disease)
Contraindications:
History of recurrent infections
Latent TB
PUD
Diabetes (worsens control)
Hypertension, heart failure
Psychiatric disorders
Glaucoma
Osteoporosis
Myasthenia gravis
