Drugs Flashcards
1
Q
what is co-amoxiclav?
A
Amoxicillin (β-lactam antibiotic)
+
clavulanic acid (β-lactamase inhibitor)
(it can overcome antibiotic resistance in bacteria that secrete β-lactamase, which otherwise inactivates most penicillins)
2
Q
what is the mechanism of action for co-amoxiclav?
A
- Amoxicillin inhibits formation of peptidoglycan cross links in bacterial cell wall.
- Clavulanic acid prevents the survival of β-lactamase enzyme which is produced by the bacteria.
3
Q
what is botulinum toxin used for?
A
achalasia
4
Q
how does botulinum work?
A
- Inhibits the calcium dependent release of ACh from the presynaptic neurones.
- This relaxes the Lower Oesophgeal Sphincter.
5
Q
what are antacids? what used for? contraindications? side effects?
A
- magnesium/aluminium salts
- dyspepsia (indigestion)
- Contraindicated for patients with renal insufficiency.
- Magnesium = laxative
- Aluminium = constipation
6
Q
what is the mechanism of action for antacids?
A
Direct neutralisation of gastric acid inside the duodenum.
7
Q
what are examples of PPIs?
A
- Omeprazole/ Lansoprazole, Pantoprazole, Rabeprazole sodium
- Esomeprazole (Nexium) - second generation PPI (S-isomer only)
8
Q
what are PPIs used for?
A
- Gastritis
- Gastric Ulcers
- Peptic Ulcers
9
Q
what do PPIs do?
A
Block the action of the H+,K+ -ATPase pump permanently in the gastric parietal cell by binding to its sulphydryl group.
10
Q
what are examples of histamine-2 (H2) receptor antagonist?
A
Ranitidine/ Cimetidine
11
Q
what are H2 receptor antagonists used to treat?
A
- Gastritis
- Gastric Ulcers
- Peptic Ulcers
12
Q
what is H. pylori triple therapy?
- standard and modern
A
Standard Triple Therapy (2 antibiotics +PPI)
e.g “CAP” – Clarithromycin, Amoxicillin, PPI (e,g, Omeprazole)
Metronidazole can be used instead of Amoxicillin.
Modern Bismuth-Based Regimens (2 antibiotics + Bismuth compound)
e.g. “CAB” - Clarithromycin, Amoxicillin, Ranitidine Bismuth Citrate
Metronidazole can be used instead of Amoxicillin.
13
Q
what is mechanism of action of omeprazole? what activated by? what is MAO of clarithromycin? what is MAO of ranitidine bismuth citrate?
A
Omeprazole - irreversible H+/K+ proton pump inhibitor (PPI). Activated by acidity, specific to canaliculi of parietal cells.
Clarithromycin – inhibits translation during bacterial DNA synthesis.
The H2 antagonist ranitidine combined with a bismuth compound both coat the gastric mucosa and help reduce HCl secretion.
14
Q
what is used for patients allergic to penicillin?
A
metronidazole
15
Q
what is pancreatin? what used for? other name? what enhanced by?
A
- Mixture of enzymes produced by exocrine pancreas e.g. amylase, lipase and trypsin.
- Chronic pancreatitis
- Cystic fibrosis
- Creon (pancrelipase)
- PPI
16
Q
what is fluorouracil (5-FU)? what used for?
A
- Pyrimidine analog
- Thymidylate synthase inhibitor
- Anti-metabolite
- CRC
17
Q
what is the MAO of 5-FU?
A
- Prevents pyrimidine from incorporating into DNA during ‘S’ phase.
- Drug is converted to a ‘fraudulent’ nucleotide called FDUMP and inhibits thymidylate synthase preventing the conversion of 2’-deoxyuridylate (DUMP) to 2’-deoxythymidylate (DTMP) resulting in ↓DNA synthesis = cell death.
18
Q
what is folinic acid also caused? what molecule?
A
leucovorin
- calcium/sodium folinate
19
Q
what is folinic acid used for?
A
- Enhance effect of 5FU (stabilise bond of 5-fdUMP to thymidylate synthetase)
- Counteract cytotoxic drug methotrexate (which is a folic acid antagonist)
20
Q
what is the MAO of folinic acid?
A
- ↑Tetrahydrofolate for 5FU to bind with and ↑ stability of 5FU-thymidylate synthase complex = ↑cytotoxicity.
21
Q
what is PEG-interferon alpha2A?
A
antiviral
- Chronic Hep B
- Chronic Hep C
- Acute Hep C (works in 85% of cases)
22
Q
what is MAO of PEG-interferon alpha2A? how administered? why PEG?
A
- Binds to cell surface receptors on virally infected cells and interferes with the viral mRNA translation.
- Proteins that interfere with viral replication and activate other immune cells.
- Given as injection.
- Can be pegylated to ↑ half-life.
23
Q
what is another old drug used for chronic hep C?
A
ribavirin
24
Q
what is the MAO of ribavirin?
A
- Inhibits viral RNA dependent RNA polymerase enzyme, therefore inhibiting viral replication.
- RNA mutagen, giving a defective HCV.
- Given as an oral tablet.
25
what are the different types of insulin? how long does each last?
```
6 Insulin Rapid-Acting (lispro)
Short-Acting (regular)
Intermediate-Acting (NPH)
Long-Acting (glargine/detemir)
Pre-mixed (short + intermediate)
```
RA – 3-5 hrs (covers meal with injection)
SA – 5-8 hrs (covers meals within 30-60 minutes)
IA – 18-24 hrs (half a day/full night, used with RA/SA)
LA – up to 24 hrs (full day with RA/SA)
Pre-mixed – taken 2/3 times a day before meals.
26
what type of drug is metformin what for? what does it do?
- Biguanide
- Insulin sensitisers
- First line DRUG for Type II diabetes.
27
what is the MAO of metformin?
- Activates AMP kinase which is involved in GLUT4 metabolism.
- ↓gluconeogenesis in liver
- ↑ peripheral glucose uptake (GLUT4)
28
what is example of sulfonylureas? what do they do?
- Gliclazide (X-amide/X-azide)
| - (increased insulin secretion)
29
what is the MAO of Gliclazide?
- Activates sulfonylurea receptors which inhibits ATP-sensitive K+ channels -> ↑intracellular K+ -> depolarisation and Ca2+ influx -> insulin release
30
what are examples of thiazolidinediones? what also called? what are they?
- (Rosiglitazone,) pioglitazone etc.
- Glitazones
- (insulin sensitisers) = increase sensitivity of cells to insulin
- PPARgamma agonists
31
what is the MAO of thiazolidinediones? side effects?
- Interaction with peroxisome proliferator-activated receptor-gamma (PPAR-gamma), mainly found on adipose cells. This increases adipogenesis and glucose uptake.
- May lower free fatty acids promoting glucose uptake by muscles.
- Lower blood glucose but do not return to normal.
- Weight gain of 5-6kg
- Oedema
- Hypoglycaemia
- Redistribution of fat from central adiposity to peripherals.
32
what are DDP-4 inhibitors used in? what example?
type II diabetes
- Sitagliptin
(X-gliptin)
33
what is the MAO of DDP-4 inhibitors?
The DPP-4 enzyme degrades incretins such as GLP-1, thus reducing insulin secretion. Hence DDP-4 inhibitors increase the action of incretins, thereby increasing insulin secretion and reducing glucagon secretion.
34
what are two of the most important incretins?
glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP).
35
what is X-tide an example of?
GLP-1 Receptor Agonists
36
what do GLP-1 receptor agonists do?
Acts as a functional analog of GLP-1, thus increasing insulin and reducing glucagon secretion.
37
what are SGLT2 inhibitors used for? what is an example?
- type II diabetes and diabetic kidney disease
| - X-gliflozin
38
what is the MAO of SGLT2?
Reduction of glucose reabsorption in the kidney, reducing blood glucose levels.
Inhibition of SGLT2 (Sodium/Glucose cotransporter in the proximal tubule), preventing glucose reabsorption, allowing glucose to be passed out in the urine
39
what are alpha-glucosidase inhibitors? what used for?
- Miglitol, Acarbose, Voglibose, Deoxynojirimycin
| - type II diabetes
40
what is MAO of alpha-glucosidase inhibitors? side effects?
Prevent digestion of carbohydrates into monosaccharides, preventing food from increasing blood glucose levels.
Competitive inhibitor of alpha-glucosidase enzymes found in the small intestinal brush border, slowing carbohydrate digestion.
- Flatulence and diarrhoea (bacterial digestion of carbohydrates)
41
what is an example of an osmotic diuretic? what indication for use?
mannitol
- ↑ICP/cerebral oedema
- ↑intraocular pressure
42
what is the MAO of osmotic diuretics?
- Act on parts of nephron freely permeable to water e.g. proximal tubule, descending limb and collecting duct.
- Inert substance which ↑osmolarity of the filtrate and reduces passive reabsorption of water.
43
what are examples of loop diuretics? what indication for use?
Furosemide, bumetanide
- Oedema
- Resistant hypertension
44
what is the MAO of loop diuretics? what is to note about these?
- Act on thick ascending loop of Henle.
- Inhibit the Na+/Cl-/K+ transporter by attaching to the Cl- binding site.
- These ions can therefore not be reabsorbed, as a result a hypotonic renal medulla is not formed and water remains in collecting duct.
- Mg2+ and Ca2+ reabsorption is dependent upon the reabsorption of the other ions these are also lost in urine.
- ↑ potassium intake should be encouraged.
- Most powerful diuretic.
45
what example of thiazide diuretic? what indication for use?
Bendroflumethiazide
- Mild/moderate heart failure.
- Hypertension
46
what is the MAO of thiazide diuretics?
- Act on distal convoluted tubule.
- Block Na+/Cl- symporter by attaching to Cl- site, hence preventing their reabsorption.
- Also ↑ reabsorption of Ca2+ by increasing activity of Na+/Ca2+ antiport.
- K+ and H+ are lost due to activation of RAAS.
- ↑ potassium intake should be encouraged.
47
what are examples of K+ sparing? when used?
- Triamterene, amiloride
- oedema
- heart failure
- adjunct with loop/thiazide
48
what is the MAO of K+ sparing?
- Act on collecting ducts and tubules.
| - Inhibit Na+ reabsorption by blocking lumenal channels and ↓K+ excretion.
49
what are examples of aldosterone antagonists? what are these also called? what used for? what do they act on?
- spironolactone, eplerenone
= potassium-sparing diuretics (increase risk of hyperkalaemia)
- on principal and alpha-intercalated cells
- oedema/ascites
- heart failure
- primary hyperaldosteronism
50
what are finasteride and dutasteride examples of? what used for?
5α-reductase inhibitor
(finasteride is selective for type II, dutasteride for I and II)
= anti-androgens
- BPH
- Male-pattern baldness
51
what is MAO of 5alpha-reductase inhibitors? side effects? effect on PSA?
- block enzyme 5alpha-reductase type 2
- prevents metabolism of testosterone into dihydrotestosterone which is indicated in causing prostate enlargement.
- decrease growth of stromal and epithelial prostate cells
- increase apoptosis
- decrease PSA (to do with hormone stuff)
- maintain improvement of symptoms
- Impotence
- ↓libido
- Ejaculation disorders
52
what are alpha-1 blockers also? what are alpha-1 blocker examples? what for? effect on PSA?
- alpha1-andrenergic antagonists
- Tamsulosin, alfuzosin, doxazosin, terozasin (Tamsulosin selective for alpha-1a subtype (and alpha-1b?) specific to bladder neck/prostate/urethra)
- BPH
- Kidney stones
- no effect on PSA
53
what is the MAO of tamsulosin?
- Inhibit the alpha 1/1a receptors resulting in relaxation muscles of bladder neck = ↑ urinary flow and ↓pain.
54
what are examples of thyroid hormone inhibitors? what used for?
Carbimzaole/ Methimazole/ Propylthyiouracil (PTU) = THIOUREYLENES
- Pro-drug for methimazole
- Thyroid hormone inhibitor
- Mild immunosuppressant
- for hyperthyroidism
55
what are the MAO of methimazole and PTU?
- Prevents thyroid peroxidase from iodinating and coupling tyrosine, therefore reducing hormone production.
- Partly blocks coupling of two iodinated tyrosines
- PTU: reduces the conversion of T4 to T3 in the peripheral tissue.
Quickly reduces hormone production however takes 10-20 days for clinical benefit due to high half lives of existing T4/T3. Hence β-blocker can be used for rapid symptom control.
56
what other medications used for hyperthyroidism?
- thyiocyanate ions
- iodide ions
- radioiodine I-131 (first-line treatment for hyperthyroidism)
57
what is the MAO of thyiocyanate ions?
- Reduces iodide trapping by competitive inhibition of the Na+/I- symporter
58
what is the MAO of iodide ions?
- Given in high concentrations
- Reduces thyroid function.
- with KI
59
what is the MAO of radioiodine I131?
- Absorbed by thyroid.
- Emits beta and gamma radiation.
- Beta radiation kills thyroid follicle cells.
60
what is propranolol? what used for? MAO? what is to note?
- Non-selective β-blocker
- treat side effects of hyperthyroidism (used while thioureylenes or radioiodine takes effect)
- Hypertension
- Anxiety
- Blocks adrenaline and noradrenaline at β1 and β2 adrenergic receptors.
- Crosses BBB therefore may have psychological effects e.g. vivid dreams, psychoses
61
what used to treat hypothyroidism? what is it?
- Levothyroxine
| - Synthetic hormone to replaces deficient T4 .
62
what are examples of antibiotics?
- tetracycline
- clarithromycin
- amoxicillin
- metronidazole
- fluoroquinolone
- sulphonamides
63
what is misoprostol?
prostaglandin analogue
64
what are examples of antacids?
- ranitidine bismuth citrate
- bismuth citrate
- bismuth subsalicylate
- sodium carbonate
- calcium carbonate
65
what is the weight-loss drug?
orlistat - blocks gastric and pancreatic lipase
66
what are P-CABs?
potassium competitive acid blockers
67
what do bismuth compounds and P-CABs do?
- Potassium competitive acid blockers (P-CABs) in development (& use in the Far East)
=faster onset and longer lasting but more reversible
- It’s all to do with pH!
- H. pylori tolerates very acid pH but only grows/divides at less acid pH (>5.5)
- Clarithromycin, amoxicillin & tetracycline all work best in dividing cells
- PPIs reduce acidity, enhancing antibiotic action (new P-CABs may give a longer lasting high pH)
- Bismuth blocks H+ influx into H. pylori so enhance antibiotic action even as the effects of PPIs are diminishing with time
68
what is ezetimibe?
- inhibits endocytosis of cholesterol
| - lowers cholesterol levels
69
what is levamisole?
used with fluorouracil
70
what is methotrexate?
folic acid antagonist (chemotherapy agent)
71
what is avastin (bevacizumab)?
VEGF-inhibitor - treat angiogenesis
72
what is pembrolizumab? what does it do?
- antibody used in cancer immunotherapy
| - blocks PD-1
73
what are 5-HT3 antagonists?
anti-emetics (chemotherapy)
74
what is naloxone?
opioid receptor antagonist -> increase motility and secretion
75
what is an opioid receptor agonist? what used for?
imodium/loperamide = decrease frequency of diarrhoea
76
what is lomotil? what used for?
- used to treat acute and chronic diarrhoea
- diphenoxylate (opioid) and atropine (muscarinic agonist)
- decrease peristalsis, decrease gastric emptying
77
what are enkephalinase inhibitors?
substances that enhacne action of enkephalins
78
what is oxaliplatin? what used with? how work?
chemotherapy drug
- often used with 5-FU and folinic acid
- interferes with development of DNA
79
what class of antivirals used for hep B? what also used for?
nucleoside (analogue) reverse transcriptase inhibitors (NRTIs)
- also for used for HIV
80
what are examples of NRTIs?
- lamivudine (3TC)
- adefovir
- entecavir
- tenofovir
81
what is the new treatment for hep C?
DAAs (direct-acting antivirals) (four classes)
82
what is a commonly used DAA? how does it work?
sofosbuvir = nucleoside & nucleotide NS5B polymerase inhibitor
They directly target the hep C virus to stop it from making copies of itself in the liver. They attach themselves onto the genetic information, called RNA, to block the virus from multiplying.
83
what is another class of DAA?
```
NS3/4A Protease Inhibitors (PIs)
- Telaprevir
- Boceprevir
(these were first DAA that were approved)
- Simeprevir
```
84
what is old treatment for hep C?
- PEG-INF
- ribavirin = not used with PEG-INF anymore (still used with Sofosbuvir)
= ribavirin = antiviral nucleoside analogue
- Ribavirin is phosphorylated to ribavirin triphosphate and is a substrate for many viral RNA-directed RNA polymerases (RdRps)
85
what does interferon do in hep B?
get rid of cccDNA
86
what is the treatment for hep D?
- PEG-INF > 48 weeks
| - not antiviral drugs for this
87
what is viagra?
phosphodiesterase 5 inhibitor (PDE5i) -> relax blood vessels
88
what used to treat an overactive bladder?
anticholinergic
89
what used to treat polycystic kidney disease?
vasopressin receptor antagonist
90
what is ADT treatment? what included in it?
androgen deprivation therapy
- GnRH agonists (e.g. Leuprolide and Goserelin) - pre-treatment with anti-androgen
- GnRH antagonist (e.g. Degarelix) - initial treatment then transfer to agonist
91
what is used for metastatic prostate cancer?
- chemotherapy -> docetaxel, cabazitaxel
| - hormone therapy -> abiraterone
92
what does abiraterone do?
CYP17 inhibitor
93
what is used to treat bone cancer?
radium 223
94
what are the anti-thyroid substances?
- thiocyanate ions
- thioureylenes
- iodide
- radioiodine I-131
95
what is the treatment for hypoadrenalism?
(Addison's disease)
- hydrocortisone
- fludrocortisone (mineralocorticoid replacement)
96
what medication used for Cushing's syndrome?
cortisol production inhibitors:
- metyrapone
- ketoconazole
- mitotane
97
what used to treat phaeochromocytoma?
- alpha-blocker (phenoxybenzoamine)
| - beta-blocker (propranolol)
98
what used to treat diabetic nephropathy?
blood pressure
- ACE inhibitors
- Losartan - angiotensin-2 receptor blockers
- Aliskeren - renin-inhibitors
99
what is salicylate? what effect?
aspirin - reverse insulin resistance
100
what is the treatment intensification for hypertension in diabetes?
ACD
A = ACE inhibitors
C = calcium channel blockers
D = diuretics
101
what's en example of an ACE inhibitor?
ramipril
102
examples of NSAIDs
apirin, diclofenac, ibuprofen
103
what are the different insulin secretagogues?
- sulfonylureas
- meglitidines
- DPP4 inhibitors
- GLP-1 receptor agonists
104
what are the insulin sensitisers?
- thiazolidinediones
| - biguanides
105
what are the other drugs for diabetes?
- insulin
- alpha-glucosidase inhibitors
- SGLT2i
106
what do biguanides do?
- decrease hepatic glucose production
| - increase muscle cell sensitivity to insulin
107
benefits side effects of biguanides?
- no hypoglycaemia
- no weight gain
- vitamin B12 deficiency
108
what do sulfonylureas do?
increase insulin secretion
109
what are side effects of sulphonylureas?
- hypoglycaemia
| - weight gain
110
what do thiazolidinediones do?
increase insulin sensitivity
111
what are advantages and side effects of thiazolidinediones?
- no hypoglycaemia
| - weight gain
112
what do DPP-4 inhibitors do? example
- increase insulin secretion (glucose-dependent)
- decrease glucagon secretion (glucose dependent)
- gliclazide
113
what is advantage of DPP-4 inhibitors?
- no hypoglycaemia
114
what do GLP-1 receptor agonists do? example?
- increase insulin secretion (glucose-dependent)
- decrease glucagon secretion (glucose dependent)
- slows gastric emptying
- increase satiety
- exenatide, lixisenatide, liraglutide)
115
what are advantages of GLP-1 receptor agonists?
- no hypoglycaemia
| - weight reduction
116
what does insulin do?
- increase glucose disposal
| - decrease hepatic glucose production
117
what are side effects of insulin?
- hypoglycaemia
| - weight gain
118
what do meglitinides (glinides) do?
increase insulin secretion
119
what are side effects of meglitinides?
- hypoglycaemia
- weight gain
- not very population – because very short acting drugs – they act similar to sulfonylureas
120
what do alfa-glucosidases inhibitors do?
- slow intestinal carbohydrate digestion/absorption
| - blocks the amylases and carbohydase enzymes
121
advantages and side effects of alfa-glucosidase inhibitors?
- no hypoglycaemia
| - GI side effects = not very popular
122
SGLT2i what do they do?
- increase glucose excretion from kidneys
| - lower threshold for glucose urine secretion
123
advantages and side effects of SGLT2i?
- insulin independent mechanism
- diuretic effect
- thrush
