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