Block 34 Pharm Flashcards
Anti-proliferative agents?
azathioprine and cyclophosphamide
Calcaneurin inhibitors?
Ciclosporin and tacrolimus
Drugs used in transplant immunosuppession?
- ciclosporin
- tacrolimus
- azathioprine
Cyclophosphamide uses?
treatment of immune based renal disease i.e. Wegener’s granulomatosis, types of glomerulonephritis or SLE
Azathioprine mechanism?
- metabolised to mercaptopurine
- purine synthesis inhibition
- inhibits B and T cells
Cautions of azathioprine?
reduce dose in elderly and TMPT activity
Azathioprine interactions?
- allopurinol
- BCG
- febuxostat
Side effects of azathioprine?
- bone marrow depression
- leucopenia
- infections
- thrombocytopenia
- pancrwatitis
Screening w azathioprine?
TMPT activity - increased risk of myelosuppression w reduced TMPT activity
cyclophosphamide mechanism?
- alkylating agent
- used to treat lymphomas and leukemias
- attaches to alkyl groups, fragmenting DNA
- DNA damage by forming cross links
- mispairing the nucleotides leading to mutations
cautions of cyclophosphamide?
- acute porphyrias
- DM
- haemorrhagic cystitis
- previous or concurrent mediastinal irradiation—risk of cardiotoxicity
interactions of cyclophosphamide?
- BCG
- vaccines
side effects of cyclophosphamide?
- alopecia
- agranylocytosis
- haemolytic uraemic syndrome
- sperm abn
cyclosporin mechanism?
- IS
- calcaneurin inhibitor that inhibits T cell activation
Tacrolimus mechanism?
calcaneurin inhibitor
CI of cyclosporin?
- malignancy
- uncontrolled HTN
- infections
Ciclosporin interactions?
- aliskiren
- amiodarone
- atorvostatin
- vaccines
side effects of ciclosporin?
- eye inflammation
- decreased appetite
- HTN
- hyperuricaemia
- renal impairment
- peptic ulcer
tacrolimus CI?
- malignant skin lesions
- infection
- cautions: avoid UV light
Tacrolimus interactions?
- amiodarone
- BCG
- cobicstat
- clarithromycin
SE of tacrolimus?
- inc infections
- skin reactions
- sensation abn
- peripheral neuropathy
- alopecia
tacrolimus in children?
cardiomyopathy - inc risk
Oxybutynin mechanism?
- antimuscarinic
- reduces detrusor activity, relaxing bladder
- prevents urge to void
oxybutynin is used for
OAB
CI for AMs like oxybutynin?
- closed angle glaucoma
- GI obstruction
- MG
- paralutic ileus
- sig bladder outflow obst
- urinary retention
side effects of all antimusacrinics?
- const
- dry mouth
- dizziness
- flushing
- headache
- urinary disordrers
oxybutynin side effects?
- diarrhoea
- dry eye
muscarinic receptor antagonists?
Oxybutinin & Tolterodine
Use of antimuscarinics?
Overactive bladder syndrome, urge predominant incontinence
Tolteridone is a ?
AM
Cautions of tolerodine?
QT prolongation
SE of tolterodine?
- bronchitis
- parasthesia
- peripheral oedema
- parasthesia
Alpha1-adrenoceptor antagonists?
Doxazosin and tamulosin
Doxazosin and tamulosin used for?
BPH
Doxazosin mechanism?
- alpha 1 adrenergic receptor antagonist
- antagonism causes smooth muscle relaxation in the prostate and bladder, effectively relieving urinary frequency, urgency, weak urinary stream,
Tamulosin mechanism?
- alpha receptor blocker
- relaxes SM in the prostate allowing urine to flow
Doxazosin CI?
- Postural hypotension
- history of micturition syncope
- monotherapy in ppts w overflow bladder
interactions of D?
- Slidenafil and avanafil
side effects of doxazosin?
- arrythmias
- cystitis
- dry mouth
- oedema
Tamsulosin interactions?
- slidenafil
Tamsulosin CI?
- micturition syncrope
- hisory of postural hypotension
SE of tamsulosin?
dizziness and sexual dysfunction
Dutasteride mechanism?
inhibitor of the enzyme 5α-reductase, which metabolises testosterone into the more potent androgen, dihydrotestosterone.
SE of dutasteride?
breast disorders, sexual dysfunction
Finasteride Mx?
inhibitor of the enzyme 5α-reductase, which metabolises testosterone into the more potent androgen, dihydrotestosterone.
Finasteride safety info?
suicidal thoughts and depression
cautions of finasteride?
obstructive uropathy
SE of finasteride?
sexual dysfunction
What are the 5-AR inhibitors?
Finasteride and dutasteride
Antimicrobial agents for urinary infections ?
- Trimethoprim (UTI)
- Nitrofurantoin (UTI)
- Co-amoxiclav (pyelonephritis)
- Ciprofloxacin (pyelonephritis)
- Gentamicin (serious gram -ve infections)
Drugs used for UTIs?
trimethoprim and nitrofurantoin
Drugs used for Pyelo?
ciprofloxacin and Co-amoxiclav
Drugs used for severe gram - UTI?
gentamicin
Trimethoprim?
- dihydrofolate reductase inhibitor preventing synthesis of nucleic acids
- bacteriacidal activioty
CI of trimethoprim?
blood dyscrasias
Cautions of trimethoprim?
acute porphyrias, predisposition to folate def
Int of trimethoprim?
- azathioprine
- clozapine
- methotrexate
- warfarin
SE of trimethoprim?
- diarrhoea
- electrolyte imbalance
- headache
- skin reactions
trimethoprim can cause?
- agranulocytsosis
- angiodema
- haemolysis
Trimethoprim is a ?
teratogen. Risk in T1
nitrofurantoin mechanism?
- inhibit the citric acid cycle as well as synthesis of DNA, RNA, and protein
- rapidly reduced to produce reactive intermediates that attack DNA
nitrofurantoin safety info?
resp symptoms and acute pulmonary reactions
CI of nitrofurantoin?
- GDP6 deficiency
- acute porphyrias
cautions of nitrofurantoin?
- DM
- folate def
- vitamin B def
- pulm disease
SE of nitrofurantoin?
- agranulocytosis
- angiodeme
- aplastic anaemia
- pulm reaction
Nitrofurantoin - avoid at?
term - can produce neonatal haemolysis
Co-amoxiclav mechanism?
- inhibits PBP preventing corss linkage of subunits
- clauvanic acid: beta lactamse inhibitor used to enhance effectiveness of beta lactams
CI of co-amox?
- history of co-amoc assoc jaundice or hepatic dysfunction
- history of penicillin assoc jaundice or hepatic dysfunction
Cautions of co-amox?
- ALL - risk of rashes
- CLL - rashes
- hydration
interactions of co-amox?
methotrexate
SE of co-amoxiclav?
diarrhoea, hypersen, skin reactions, thrombocytopenia
common side effect of co-amox?
inc risk of infection, diarrhoea
ciprofloxain is a ?
quinolone
TWO
CI of quinolones?
- QT prolongation
- UV exposure
- GPD6 def
side effects of quinolones?
- dec appetite
- asthenia
- constipation
- QT prolongation
- peripheral neuropathy
- C diff
ciprofloxacin mechanism?
- bacterial topoisomerase II (DNA gyrase) and 4
- Targeting DNA gyrase prevents supercoiling the DNA
gentamicin mechanism?
- aminoglycoside
- 30s ribosome inhibition
CI of aminoglycosides?
- MG - they impair NM transmission
- auditory disorders
SE of all aminoglycosides?
- aphonia
- bronchospasm and cpigh
- haemoptysis
- RI
Imp side effects of AG?
- ototoxicity
- nephrotoxicity - occurs more w RI
Phosphodiesterase type 5 inhibitors?
- Sildenafil & Tadalafil
- for Erectile dysfunction
Slidenafil and Tadalfil mechanism?
- PDE-5 inhibition
- leads to SM relaxation - vasodilation
Slidenafil CI?
- recent MI or stroke
- degenerative retinal disorders
- hypotension
cautions of slidenafil?
- active peptic ulceration
- autonomic dysfunction
- bleeding disorders
- myeloma
slidenafil interactions?
- clarithromycin
- cobicstat
- doxazosin
- GTN and other vasodilators
SE of slidenafil?
- alopecia
- GI disorders
- infection
- night sweats
- vasodilation
Tadalafil CI?
- acute MI
- hypotension
- optic neuropathy
- HF
- recent stroke
tadalafil SE?
- flushing
- GI discomfort
- headaches
- nasal congestion
alprostadil mechanism?
- Prostaglandin E1 agonist
- relaxes SM
- promotes vasodilation
Humulin-S ?
quick acting human insulin
Insulin lispro?
analogue quick acting
Insulin aspart?
analogue quick acting
Insulatard?
human iosphane
Humulin M3?
Human biphasic
Humalog Mix25?
analogue biphasic
Insulin glargine?
anologue long acting
Insulin degludec?
analogue long acting
insulin mechanism?
- promotes glucose and AA uptake into muscle and adipose tissues
- except liver and brain
- inhibits gluconeogenesis in the liver
- anabolic role in stimulating glycogen, FA and protein synthesis
insulin interactions?
- clarithromycin
side effects of all insulins?
- oedema
- lipodystrophy
Sulfonylureas?
- Gliclazide
- Glimepiride
Glicazide mechanism?
- binds to the SUR1 receptor blocking ATP sensitive k+ channels
- decreased potassium eflux -> depolarisation of b cells
- exocytosis of insulin granules
glimepiride?
- SU
- promotes insulin secretion by binding to potassium channels
CI of all sulfonreas?
Ketoacidosis
cautions of all sulfonylureas?
- elderly
- can cause weight loss
- GDP6 def
side effects of all SU?
- abd pain
- diarrhoea
- hypoglycaemia
- nausea
- agranulocytosis
Meglitinides?
Repaglinide
Repaglinide mechanism?
- potentiates the effect of EC glucose on K+ channels
- closes K+ channels, depolarising B cells, opening Ca+ channels, causing calcium influx -> insulin secretion
CI of Repaglinide?
ketoacidosis
Repaglinide interactions?
clopidogrel
side effects of Repaglinide?
- abd pain
- diarrhoea
- hypogly
Metformin mechanism?
- decreasing gluconeogenesis in hepatocytes
- increases peripheral utilisation of glucose
CI of metformin?
- acute metabolic acidosis - lactic acidosis and DKA
metformin - RF for lactic acidosis?
- chronic hF
- drugs that impair renal function
- interrupt tx if dehydration occurs
- tissue hypoxia
Long term use can lead to…
metformin SE?
- abd pain
- dec appetite
- diarrhoea
- b12 def
- lactic acidosis
GI side effects of metformin?
Gastrointestinal side-effects are most frequent during treatment initiation and usually resolve spontaneously. A slow increase in dose may improve tolerability.
biguanide =
metformin
Thiazolidinediones =
pioglitazone
pioglitazone mechanism?
- PPAR agonist -> transcription of insulin genes
- reduces hepatic gluconeogenesis
- in adipose tissues, skeletal muscle and liver
- reduced peripheral resistance to insulin
pioglitazone safety info?
- HF espec when past MI
- risk of bladder cancer
CI of pioglitazone?
- DKA
- HF
- prev/ active nladder cancer
cautions of pioglitazone?
- use w insulin - risk of HF
- risk of bC
- Elderly
interactions of pioglitazone?
- clopidogrel
side effects of pioglitazone?
- bone factures
- infections
- numbness
- increased weight
- bladder cancer
How does this drug class work?
Linagliptin?
- DPP-4 inhibitor -> slows breakdown of GLP-1 and GIP
- GLP1 and GIP stimulate insulin release and prevent glucagon release
linagliptin is not
affected by renal impairment
DPP4 inhibitorS?
- Linagliptin (not affected by renal function) – Sitagliptin
- Saxagliptin
cautions of linagliptin?
pancreatitis
SE of linagliptin?
- angioedema
- cough
- nasopharngitis
- panc
Saxagliptin SE?
- abd pain
- fatigue
- panc
- vomiting
- angioedema
Side effects of sitagliptin?
- renal impairment
- acute panc
- angioedema
- headache
Acarbose mechanism?
- inhibitor of alpha glucosidases and amylase
- delays and prevents digestion and abs of starch and carbs -> reducing BG
CI of acarbose?
- hernia
- IBD
- malabs
- intestinal obst
cautions of acarbose?
- can enhance hypoglycaemia when used w insulin and SU
Hypoglycaemia with acarbose is treated w?
oral glucose but not sucrose
side effects of acarbose?
- Diarrhoea
- GI discomfort
- GI disorders
ɑ-Glucosidase inhibitors =
acarbose
SGLT2 inhib?
- Canagliflozin
- Empagliflozin
SGLT2 inhib mechanism?
- SGLT2 found in PCT
- inhibition lowers reabs of flitered glucose in the body -> inc glucose excretion in urine
Canagliflozin safety info?
- DKA
- lower limb amputation
- Fournier’s gangrene
CI of canagliflozin?
- DKA
- T1D - inc DKA risk
SE of canagliflozin?
-const
- dyslipidemia
- hypoglycaemia - when used w insulin or SU
- infections, urosepsis
empagliflozin CI?
- dka
- t1d
side effects of empagliflozin?
- const
- hypo
- hypovolaemia
- fourner’s gangrene
- urosepsis
Glucagon like peptide-1 (GLP-1) mimetics
- Dulaglutide
- Liraglutide
- Semaglutide
Dulaglutide action?
- helps glucose dependent insulin secretion
- slows gastric emptying
GLP-1 analogues safety info?
- DKA when used w insulin especially on discontinuation of insulin
CI of dulaglutide?
severe GI disease
SE of dulaglutide?
- appetite decreased
- const
- hypoglycaemia
- GB
- acute panc
CI of liraglutide?
- IBD
- diabetic gastroparaesis
SE of liraglutide?
- asthenia
- const
- GB disorders
- panc
semaglutide=
ozempic
semaglutide CI?
DKA, pancreatitis
SE of semaglutide?
- cholethiasis
- hypoglycaemia when used w other drugs
- weight loss
- panc
glucagen hypokit=
- glucagon
CI of glucagen hypokit (glucagon)
- starvation
- adrenal insufficiency
- glucagoma
interaction of glucagen hypokit?
warfarin
SE of glucagen hypokit?
- nausea
- vomiting
- tachycardia, HTN, hypotension
glucagon mechanism?
- raised BG through activation of hepatic glucagon receptors stimulating glycogenolysis and release of glucose
when is glucagon used?
hypoglycaemia
IV Glucose =
Intravenous 20% Glucose
glucose cautions?
- prolonged use can lead to hyponatreamia
SE of glucose?
- chills
- electrolyte imbalance
- venous thrombosis
- polyuria
glucose mechanism?
- converted to fat -> energy source
- in liver and muscles -> glycogen
Carbamazole safety info?
- neutropenia and agranulocytosis
- congenital malformations
- risk of acute panc
SE of carbimazole?
- bone marrow disorders
- haemolytic anaemia
- SCARs
- angranulocytosis
carbimazole mechansim?
- decreases iptake of iodine by thyrpid
- prevents thyroid perioxidase from iodinating tyrosine residues on thyroglobulin
-> red production of T3 and T4
Thionamides =
- Carbimazole
- Propylthiouracil
proprylthiouracil mechanism?
- binds to thyroid perioxidase inhibiting conversion of iodide to iodine
- inhibts production of new thyroid hormones
propylthiouracil SE?
- agranulocytosis
- BM disorders
- glomerulonephrotis
- hearing impairment
- hepatic reactions
which thionamide is safe in pregnancy?
PTU
B blocker used for hyperthyroidism?
propanolol
Radioiodine and oral iodine solutions =
- Radioiodine (I131)
- Aqueos Iodine oral solution
Radioiodine I-131 indications?
Tx of hyperthyroidism and thyroid carcinomas
mechanism of radioiodine?
- iodine concentrates in thyroid via soidum/ iodide transporte
- destruction of thyroidal tissue by beta emission of sodium iodidie
radioiodine SE?
- conjunctivitis
- ED
- influenza like illness
- rash
levothyroxine CI?
thryotoxicosis
side effects of levothyroxine?
- angina
- hyperhidrosis
- palpitations
- thryotoxic crisis
- weight loss
levothryoxine mechanism?
- inc metabolic rate
- decreases TSH production
Hydrocortisone has equal?
gluco and mineralocorticoid action
hydrocortisone ix?
- thyrotoxic crisis
- adrenal insufficency
- adrenal crisis
- asthma
CI of all corticosteroids?
- live caccines in those receiving immunosppresive doses
- systemic infection
SE of all corticosteroids?
- cushings syndrome
- fluid retention
- HTN
- osteoporsis
- hirtutism
- peptic ulcr
steroids - adrenal suppression?
- prolonged use -> adrenal atrophy
- abrupt withdrawal -> adrenal insufficiency, death or hypotension
other side effects of steroids?
- psychiatric - euphoria, insomnia, mood lability, suicidal thoughts, psychotic reactions
- infections
glucocorticoids =
- Hydrocortisone
- Prednisolone
- Dexamethasone
corticosteroids mechanism?
- dec vasodilation
- inhibition of neutrophils
- inhibit phospholipase A2
prednisolone exerts…
predominantly glucocorticoid effects with minimal mineralocorticoid effects.
SE of pred?
- diarrhoea
- dyslipidaemia
- protein catabolism
dexamethasone has a….
very high glucocorticoid activity and insignificant mineralocorticoid activity.
Fludrocortisone is a
mineralacorticoid
fludrocortisone Mx?
- binds to mineralocorticoid receptors causing inc density of Na/K/ ATPase
- inc BP, inc sodium levels
- decreased plasma K+
synthetic human GH =
Somatropin
somatotropin Mx
- HGH
- stimulates prod of IGF-1, inc conc of glucose amd FFA
Somatotropin indications?
- turner syndrome
- GH def
CI of somatotropin?
- evid of tumour activity
SE of somatotropn?
- CTS
- fluid retention
- lipoatrophy
- oedema
- parasthesia
Somatotropin - fundoscopy when
Funduscopy for papilloedema recommended if severe or recurrent headache, visual problems, nausea and vomiting occur - benign intercranial hypertension
Tetracosactide =
synthetic ACTH
Tetracosactide indications?
- adrenal insufficiency
Tetracosactide CI?
- Acute porphyrias
- asthma
- cushins
- peptic ulcer
- primary adrenal insufficiency
Tetracosactide SE?
- angiodema
- fractures
- worseneed diabetes
- exopthalmus
- cushings
Tetracosactide mechanism?
- diagnosis of adrenal insufficiency
- synthetic ACTH
- in normal ppts, causes synthesis of adrenal cteroids
- doesn’t inc plasma cortisol conc w primary or secondary AI
Cabergoline mechanism?
- dopamine agonist
- D2 receptors
- Dopamine inhibits prolactin
indications of cabergoline?
- prevents and suppresses lactation
safety info w cabergoline?
- Cabergoline has been associated with pulmonary, retroperitoneal, and pericardial fibrotic reactions.
- impulse control disorders
CI of cabergoline?
- pericardial fibrosis
- psychosis
- pre-eclampsia
- peptic ulcers
cabergoline interactions?
clarithro, erythromycin
cabergoline SE?
- angina
- confusion
- sexual dysfunction
- hallucinations
D2 agonists =
Cabergoline & Quinagolide
Sustanon =
test esters
Testosterone (sustanon and testogel) ix?
androgen def
testosterone interactions?
- alc
- daleteparin
- enoxaparin
Bisphosphonates =
- Alendronic acid
- Residronate
- Zolendronic acid
bisphosphonates indications?
- post meno osteoporosis
- osteoporosis in men
bisphosphonates safety info?
- atypical femoral fractures
- osteonecrosis of the jaw and external auditory canal
CI of bisphosphonates?
- hypocal
- oesophageal abn
- strictures and achalasia
Bisphosphonates SE?
- ANAEMIA
- Oesophageal ulcer
- oesophagitis
- renal impairment
vitamin D compounds?
- Alfacalcidol (1a-hydroxycholecalciferol)
- Calcitriol (1,25-dihydroxycholecalciferol)
- Ergocalciferol (vitamin D2)”
alfacalcidol =
1a-hydroxycholecalciferol, needs activating
calcitrol =
1,25-dihydroxycholecalciferol = ACTIVATED
ergocalciferol =
vitamin D2, inactivated vitamin D
ergocalciferol Indications?
- primary prev of Vitamin D def
- treatment of vitamin D def
- hypocalcaemia of hypoparathyroidism
CI of all vitamin D analogues - calciferols?
- hypercal
- metastatic calcification
side effects of all vitamin D analogues?
- abd pain
- hypercal
- hypercalciuria
- skin reactions
symptoms of vitamin D overdose?
- anorexia
- lassitude
- nausea and vomiting
- polyuria
- thirsy
alfacalciferols Mx?
- in chronic RF, hypoparathyroidism, rickets, hydroxylation capacity is impaired
- active vitamin D so restores functions of endogenous 1,25-dihydroxyvitamin D
alfacalcidol indications?
- renal impairment requiring Vitamin D
- hypoparathyroisism
SE of alfacalcidol?
- abd discomfory
- hyperphosphataemia
- pustular rash
calcitrol Ix?
- psoriasis
- renal osteodystrophy
- PM osteoporosis
calcitrol SE?
- UTI
- drowsiness
- paralytic ileus
- polydipsia
- psychiatric disorder
vasopressin analogues?
Desmopressin and Terlipressin
desmopressin Ix?
- DI
- diagnosis of DI - water deprivation test
- Idiopathic polyuria
desmopressin CI?
- cardiac insufficiency
- hyponatreamia
- SIADH
desmopressin interactions?
lamotrigine
desmopressin side effects?
- headache
- hyponatreamia
- nausea
drug used for cranial diabetes insipidus
desmopressin
drug used for oesophageal bleeding
telipressin
bleeding reduction in mild to moderate haemophilia =
desmopressin
desmopressin mechanism?
- binds to V2 receptors, synthetic ADH
- causes increased insertion of aquaporins into the collecting duct
telipressin mechanism?
- used to treat oesophageal varices
- synthetic vasopressin analogue
- causes vasoconstriction in these vessels reducing portal pressure
telipressin safety info?
- risk of resp failure and septic shock in type 1 hepatorenal syndrome
cautions of telipressin?
- QT prolongation
- resp disease
- septic shock
- uncontrolled HTN
SE of telipressin?
- abd cramps
- HTN, hypotension
- peripheal ischaemia
- vasoconstriction
tolvaptan mechanism?
- selective V2 antagonist (vasopressin ant)
- blocks aquaporin insertion preventing water reabs
- decreases urine conc and urine osmolarity
tolvaptan CI?
- anuria
- hypernatreamia
- volume depletion
use of tolvaptan?
hyponatraemia secondary to SIADH
SE of tolvaptan?
- asthenia
- reflux
- gout
- hypernatreaia, hyperglycaemia
- hepatic disorders
tolvaptan - stop treatment if ? occurs
Interrupt treatment and perform liver-function tests promptly if symptoms of hepatic impairment occur (anorexia, nausea, vomiting, fatigue, abdominal pain, jaundice, dark urine, pruritus)
paracetamol indications?
- pyrexia
- pain
paracetamol interactions?
- alcohol
- dalteparin
- enoxaparin
- fluoxacillin
side effects of paracteamol?
- thrombocytopenia
- hypotension
- angioedema
- liver injury
paracetamol mechanism?
- COX1 and COX2 inhibition -> reduced PG syntheis -> less pain
- COX-3 inhibition
- direct effect on heat regulating centers -> peripheral vasodilation
co-codamol Ix?
pain
CI of co-codamol?
- UC
- ab assoc colitis
- ultra-rapid codiene metabolisers
codiene interactions?
- clozapine
- naltrexone
- buprenorphine
SE of co-codamol?
- abd pain
- addiction
- thrombocytopenia
- pancreatitis
NSAIDs used for
acute, chronic and neuropathic pain
CI of ibuprofen?
- active bleeding or ulceration
- Haemorrhage
- severe HF
Ibuprofen interactions?
- aprostadil
- alteplase
- apixaban
- aspirin
SE of ibuprofen?
Gi discomfort, skin reactions, rash, ulcers
ibuprofen mechanism?
- NSAID
- non selective COX-1 and COX-2 inhibitor
naproxen mechanism?
- COX-1 and COX-2 inhibition
- COX-2 inhibition -> antipyretic, anti-inflammatory, and analgesic properties
COX enzymes?
- 1 is const active, found in normal stomach lining
- 2 is inducible and produces prostaglandins that mediate pain, fever and inflammation
CI of naproxen?
- active bleeding or ulceration
- severe HF
Side effects of naproxen?
- agranulocytosis
- angioedema
- aplastic anaemia
- asthma
- ulcers
Opiod analgesics?
- acute and chronic moderate to severe pain, WHO pain ladder
- Codeine phosphate
- Morphine sulfate
- Diamorphine
- Tramadol
codiene mechanism?
- agonist of mu opiod receptor -> hyperpolarizes the neuron -> inhibits release of nociceptive NTs
- metabolised in the liver to morphine
codiene indications?
- dry or painful cough
- diarrhoea
-ST pain relief
CI of codiene?
- active UC
- ab assoc colitis
- ultra rapid metabolisers
- conditions where abd distention develops
SE of all opiods?
- constipation
- dry mouth
- hyperhidrosis
- miosis
- nausea on initiation
- urinary retention
- resp despresion
morphine mechanism?
- mu and kappa opiod receptors
- acts on NA delta opiod receptors to activate reward pathway
SE of morphone?
- insomnia
- malaise
- NM dysfunction
- asthenia
diamorphine mechanism?
- oral: FPM by liver
- crosses BBB
- mu opiod agonist -> activates descendin inihib pathways
diamorphine indications?
- acute pain
- pulm oedema
- MI
CI of diamorphine?
- delayed gastric emptying
- phaechromocytoma
Diamorphine SE?
- Biliary spasm
- circ depression
- inc ICP
- postural hypotension
tramadol mechanism?
- SNRI and centrally acting opiod
- MOR agonist
CI of tramadol?
- acute alcohol intoxication
- hypnotic intoxication
- opiod intox
- analgesic intox
SE of tramadol?
- fatigue
Non opiod non NSAID analgesics?
- Amitriptyline
- Duloxetine
- Gabapentin
- Carbamazepine
- Capsaicin
chronic and neuropathic pain
Amitryptyline Ix?
- abd pain
- depression
- neuropathic pain
- migrain prophylaxis
CI of amitryptyline?
- manic phase of bipolar
- HB
- arrythmias
SE of amitryptiline?
- anticholinergic syndrome
- QT proolongation
- drowsiness
- agranulocytosis
amitryptiline overdose?
- dry mouth
- coma
- hypotension
- hypothermia
- hyperreflexia
- resp failures
amitrip mechanism?
- TCAD
- SNRI
- increased GABA transmission through increased noradrenaline levels
Duloxetine mechanism?
SNRI reuptake inhibitor
indications of duloxetine?
- MDD
- GAD
- diabetic neuropathy
- stress UI
SE of duloxetine?
- decreased appetite
- const
- diarrhoea
- palpitations
- galactrorrgoea
gabapentin indications?
- seizures
- MS
- pain
gabapentin safety info?
- risk of suicidal thoughts
- risk of severe resp depression
cautions of gabapentin?
- DM
- substance abuse
- resp depression
SE of gabapentin?
- anx
- confusion
- HTN
- sexual dysfunction
gabapentin mechanism?
- enhanced GABA synthesis
- reduces neuropathic pain and epiliepsy
carbamazepine mechanism?
- inc GABA transmission
indications of carbamazepine?
- diabetic neuropathy
- epilepsy
- trigeminal neuralgia
- BPD
CI of carbamazepine?
- AV abn
- history of bone marrow depression
SE of carbamazepine?
siADH-> hyponatreamia
Capsaicin mechanism?
- reduces amount of substance P
- Defunctionalization of nocicpetive fibers by inducing a topical hypersensitivity reaction
Capsaicin indications?
localised neuropathic pain (topical drug)
SE of Capsaicin?
- AV block
- eye irritation
- palpitations
- peripheral oedema
alkylating agents =
Cyclophosphamide
uses of cyclophosphamide?
-Cancer chemotherapy
- Autoimmune and conective tissue disorders
cyclophosphamide cautions?
- DM
- acut porphyrias
- haemorrhagic cystitis
- prev/ concurrent mediastinal irradiation - risk of cardiotoxicity
SE of cyclophosphamide?
- agranulocytosis
- alopecia
- cystitis
- HUS
Cytotoxic antibiotics =
Doxorubicin
doxorubicin mechanism?
- interupts topoisomerase II mediated DNA repair
- generates free radicals damaging cellular membranes
doxorubicin uses?
- NHL
- acute leukemias
- BC
SE of doxorubicin?
- alopecia
- Cardiomyopathy
- BM depression
- vasodilation
anti-metabolites =
Methotrexate
Methotrexate mechanism?
- DHFR inhibitor -> prevents synthesis of purines and pyrimidines
- cancer chemo and DMARD
methotrexate indications?
- CD
- RA
- Cancer
Methotrexate safety info?
- photsensitivity reactions including phototoxicity
CI of methotrexate?
- active infection
- ascites
- immunodef
Methotrexate cautions?
- blood count - bone marrow suppression
- GI toxicity - stomatitis or diarrhoea
- photosensitivity
SE of methotrexate?
- seziures
- leucopenia
- throat ulcers
- pulm and liver toxicity
Anti-oestrogens?
- Tamoxifen
- Anastrazole
- breast cancer
Tamoxifen mechanism?
- induces gonadotropin release by occupying oestrogen receptors in hypothalamus
CI of tamoxifen?
- thromboembolism
Tamoxifen interacts w
warfarin
SE of tamoxifen?
- Embolism and thrombosis
- ischaemia
- neoplasms
- agranulocytosis
tamoxifen - risks?
- endometrial changes - prompt Ix if abnormal vaginal bleeding including menstrual irregularities, vaginal discharge, and pelvic pain
- risk of thromboembolism
Anastrazole CI?
premenopausal women, susceptibility to oestoporosis
SE of anastrazole?
- alopecia
- bone pain
- CTS
- vaginal haemorrhage
- hot flush
anastrazole Mx?
- aromatase inhibitor
- preventing synthesis of oestrogen -> stops growth of hormone receptor positive tumours
ferrous sulphate Mx?
- IDA
- transported across DMT-1 to be incorporated into ferritin
- combines w porphyrin and globin chains to form hb
safety info w iV iron?
serious hypersen and anaphylactic rractions
CI of all iron?
- dist in utilisation or iron
- iron overload
SE of all iron?
- dizziness
- flushing
- HTN
- hypophosphataemia
iron sucrose is given by
iv injection or IV infusion
Side effect of ferrous sulphate?
- constipation
- GI discomfort
- nausea
constipation w iron?
- can lead to faecal impactation
- can exacerbate diarrhoea in ppts w IBD
Monitoring w ferrous sulphate?
- monitor hb conc within first 4 weeks of treat then every 4 weeks
- once hb is within normal range, continue treatment for a further 3 months to replenish further iron stores
hydroxocobalamin mechanism?
- synthetic B12
- used to treat B12 deficiency and perinicous anaemia
hydroxocobalamin SE?
- diarrhoea
- dizziness
- hot flush
- urine discoloration
Folic acid indications?
- folate deficiency megaloblastic anaemia
- prevention of nT defects in pregnancy
- prevention of methotrexate induced side effects
cautions of folate?
Should never be given alone for pernicious anaemia or other megaloblastic anaemias caused by vitamin B12 deficiency (may precipitate subacute combined degeneration of the spinal cord)
SE of folic acid?
- abd distension
- B12 def exacerbated
- flatulence
folic acid mechanism?
- Folic acid, as it is biochemically inactive, is converted to tetrahydrofolic acid and methyltetrahydrofolate by dihydrofolate reductase (DHFR
- synthesis of purines
use of Erythropoietins?
Renal anaemia
Darbepoetin =
- EPO
- inc red cell production
- activates JAK-STAT pathway
Darbepoetin safety info?
- risk of severe cutaneous adverse reactions
- overcorrection of hb
CI of all epoetins?
- pure red cell aplasia following EPO therapy
- uncontrolled HTN
SE of all epoetins?
- embolism and thrombosis
- HTN
- stroke
- influenza like illness
darbepoetin common SE?
oedema
Antiemetics?
- Cyclizine (antihistamine)
- Hyoscine (antimuscarinic)
- Metoclopramide (dopamine receptor antagonist)
- Prochlorperazine (dopamine receptor antagonist)
- Ondansetron (5-HT3 receptor antagonist)
- Aprepitant (neurokinin 1 receptor antagonist)
- Nabilone (cannabinoid)”
Used for?
Cyclizine?
- nausea and vomiting
- motion sickness
cautions of cyclizine?
- eplipesy
- severe HF
- urinary retention
cyclizine side effects?
- dec conciousness
- agranulocytosis
- bronchospasm
- hepatic disorders
- haemolytic anaemia
cyclizine mechanism?
- h1 receptor antagonist
uses of anti-emetics?
-motion sickness, postoperative vomiting, drug-induced vomiting, cytotoxic drug-induced vomiting, pregnancy-induced vomiting
Hyoscine mechanism?
- antimuscarinic
- competitive inhibitor
Antimuscarinics (hyoscine) CI?
- Closed angle closure
- GI obst
- paralytic ileus
- urinary retention
SE of antimuscarinics?
- constipation
- dry mouth
- urinary disorders
- tachycardia
Metoclopramide mechanism?
- D2 antagonist and serotonin antagonist in the chemoreceptor trigger zone
CI of metoclopramude?
- GI obst
- GI haemorrhage
- GI perf
Side effects of metoclopramide?
- depression
- hypotension
- menstryal irreg
- parkinsonism
Metclopramide can cause ? reactions
- acute dystonic reactions involving facial and skeletal muscle spasms and oculogyric crises
- more common in women, the young and the very old
Prochlorperazine mechanism?
- D2 antagonist in the CTZ
- AP
CI of Prochlorperazine?
cns depression and comatose states
side effects of prochlorperazine?
- SIADH
- Hyponatreama
- photosensitivity reaction
Ondansetron =
- 5HT3 receptor antagonist
ondansteron safety info?
(pregnancy)
inc risk of cleft lip following use in the first 12 weeks of pregnancy
ondansteron CI?
Congenital long QT
side effects of ondansteron?
- const
- feeling hot
- sens abn
- QT prolongation
Aprepitant mechanism?
- neurokinin 1 receptor antagonist
SE of Aprepitant?
- decreased appetite
- constipation
- GI discomoft
- hiccups
Nabilone mechanism?
- cannabinoid
- CB1 receptor
Nabilone cautions?
- history of psych disorder
- adverse effects on mental state
- heart disease
Nabilone SE?
- Abd pain
- confusion
- dry mouth
- hallucination
calcium salts?
- Calcichew (oral supplement)
- Calcium gluconate (Parenteral - IV)
- Calcium chloride (Parenteral - IV)”
what are calcium salts used for?
bone disease
calcichew?
- oral
- colecalciferol
- calc carbonate
calcium gluconate indications?
- severe hypocalcaemia
- acute severe hyperkalaemia
CI of all calcium salts?
- hypercalcaemia - malignancy?
SE of calcium?
- diarrhoea
- nausea
- const
- hypercal
side effect of calcium gluconate?
- arrythmias
- circ collapse
- hypotension
- vasodilation
monitoring w calcium gluconate?
Plasma-calcium and ECG monitoring required for administration by slow intravenous injection (risk of arrhythmias if given too rapidly)
calc chloride indications?
- hyperkal >6.5
- acute severe hypocalcaemia