Pharmacology finals COPIED Flashcards

(149 cards)

1
Q

What is dipyridamole?

A

a coronary vasodilator and a relatively weak antiplatelet drug.

inhibits platelet adhesion to the vessel wall.

Used combined with aspirin.

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2
Q

what’s the Mx of an acute migraine?

A

oral triptan and an NSAID/ paracetamol

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3
Q

What is the prophylaxis mx of migraines?

(2 attacks or more per month)

A

either

Topiramate

or

Propranolol (not for asthamatics)

(pizotifen is NOT recommended)

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4
Q
A
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5
Q

mech of action,

clinical indications,

potential adverse effects
of cimetidine, famotidine, ranitidine

(histamine H2-receptor antagonists)

A

drugs compete with histamine for binding to H2 receptors on gastric parietal cells.

Reduce volume and conc of gastric acid. This also proportionally decreases pepsin. (Gastric acid is the pepsinogen-pepsin catalyst)

cimetidine - weak antiandrogenic activity; can cause gynecomastia in elderly men.

cimetidine - WELL-KNOWN - inhibits P450 enzymes, therefore care with polypharmacy.

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6
Q

mech of action,

clinical indications,

potential adverse effects
of omeprazole

(proton pump inhibitor)

A

inhibitors of proton-pump, Strong inhibitors of gastric acid

Choice drug for peptic ulcers

Choice drug for GERD

Choice drug for Zollinger-Ellison syndrome

Choice drug for long-term NSAID therapy

hypomagnesemia can occur with long-term PPI therapy.

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7
Q

mech of action,

clinical indications,

potential adverse effects
of calcium carbonate

(gastric antiacid)

A

chemically neutralize stomach acid.

Commonly used for acid indigestion and dyspepsia.

Can cause some constipation, can cause rebound acid secretion.

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8
Q

mech of action,

clinical indications,

potential adverse effects
of sucralfate,

(cytoprotective drug)

A

this polysaccharide adhers to ulcer craters , inhibits pepsin-catalyzed hydrolysis of mucosal proteins. Helps form a protective barrier.

Used to treat peptic ulcers, but not so effective as H2blockers or PPIs, so only indicated with patients who can’t tolerate the others.

Take 2 hours between other drugs.

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9
Q

mech of action,

clinical indications,

potential adverse effects
of metoclopramide

others; prochlorperazine, domperidone

(acts peripherially - prokinetic drug

and acts centrally - antiemetic)

A

Blocks dopamine D2 receptors; this prevents the relaxation of GI smooth muscle produced by dopamine. Also increases acetylcholine from cholinergic motor neurons in the enteric nervous system.

>> tone and motility in the oesophagus and stomach. (therefore opioid induced sickness)

Also >> gastric emptying.

NB> also increases resting pressure of lower oesophageal sphincter, therefore << acid reflux.

Indications: GERD, diabetic gastroparesis, intractable hiccup, also antiemetic.

Adverse effects: CNS reactions. CONTRAINDICATED with px with seizures.

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10
Q

mech of action,

clinical indications,

potential adverse effects
of psyllium

(bulk forming laxative)

A

Indigestible hydrophilic drug

absorbs water and increases mass of stool. This stimulates mech peristalsis.

Also used to treat diarrhoea

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11
Q

mech of action,

clinical indications,

potential adverse effects
of docusate sodium

(stool softener)

A

facilitate movement of water into fatty intestinal material, thus softening stool.

Indicated for hard, dry stool, prevent aggravation of haemorrhoids, helping px avoid straining.

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12
Q

mech of action,

clinical indications,

potential adverse effects
of milk of magnesia

(osmotic laxative)

A

poorly absorbed salt that osmotically attracts water.

Administer to px to evacuate the bowel in prep for surgery.

Danger> loss of fluids and electrolytes

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13
Q

mech of action,

clinical indications,

potential adverse effects
of senna, bisacodyl

(stimulant - secretory laxatives )

A

Alter fluid secretion and stimulates peristalsis

Bisacodyl; used to evacuate the bowel. Can cause cramping and electrolyte/ fluid depletion. SHORT term use only.

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14
Q

mech of action,

clinical indications,

potential adverse effects
of ondansetron

(phenothiazines)

A

Selective 5-HT3 receptor antagonist; competitively block 5-HT3 receptors. I.e. blocks stimuli from the chemoreceptor trigger zone.

Acts both peripherally and centrally (vomiting centre)

Indicated for : cancer chemotherapy-induced emesis.

Adverse effects: headache, constipation, and diarrhoa.

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15
Q

mech of action,

clinical indications,

potential adverse effects
of dronabinol

(marijuana derivatives)

A

used for cancer chemotherapy induced emesis when other drugs have failed.

Used as an appetite stimulant for anorexic HIV patients

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16
Q

mech of action,

clinical indications,

potential adverse effects
of promethazine

(antihistamine)

A

H1 Antihistamine

treats nausea and vomiting induced by medications, anesthetics, and a wide range of other stimuli.

Rectal suppository or injection.

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17
Q

Which cells secrete gastrin?

A

G cells in the stomach’s antrum

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18
Q

What hormone stimulates the parietal cells?

A

Gastrin

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19
Q

Gastrin and acetylcholine also stimulates the release of ……. from paracrine cells

A

Histamine

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20
Q

What is the relationship between histamine and gastric acid production?

A

histamine stimulates H2 receptors located on parietal cells and provokes acid secretion.

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21
Q

What is used primarily for the treatment of motion sickness?

A

Scopalamine - muscarinic receptor antagonist similar to atropine.

Been used by astronauts.

Skin patch slow 72 hr release.

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22
Q

mech of action,

clinical indications,

potential adverse effects
of misoprostol,

(cytoprotective drug)

A

Prostaglandin E1 analogue

expensive. Inhibits gastric acid secretion, promotes mucus and bicarbonate.

Primary indication: prevention of gastric and duodenal ulcers with px who take NSAIDs long term.

contraindicated in PREGNANCY (stimulates uterine contractions)

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23
Q

H. Pylori tx

A

Triple therapy

PPI + two or more antimicrobial agents

eg. amoxicillin + clarithromycin

or metronidazole + clarithromycin

5 days + 5 days treatment programme

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24
Q

What’s the treatment for GERD?

(causing oesophagitis)

A

<< gastric acidity (two main groups previously mentioned)

increase the compromised oesophageal sphincter pressure (metoclopramide)

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25
Summary peptic ulcer meds
Histamine H2 receptor antagonists, or a proton pump inhibitor, or a cytoprotective agent + antibiotics for H.pylori
26
Diagram of vomiting pathways
28
Treatment of **Crohn's**
Control flare-ups **steroids, immunosuppresants** (eg. **azathioprine**) otherwise **biological agents**; **infliximab** (targets TNF) Surgery
29
ranitidine
**H2 histamine receptor antagonist** blocks histamine and thus decreasing the amount of acid released by cells of the stomach.
30
What is **mesalazine** used for? (5-aminosalicyclic acid) 5-ASA
treatment of choice for maintenance of **mild-to-moderate ulcerative colitis**. (also reduces risk of colorectal cancer) Also used inconjunction with **antibiotics** for the treatment of **diverticulitis**.
31
What is **Hyosine** used for? | (and MOA)
Motion sickness and vesibulocochlear dysfunction. Targets the vomiting centre and vestibulocochlear nuclei.
32
How does cyclizine work and indications?
**Histamine (H1) receptor antagonist** Targets the vestibulocochlear nuclei **Labyinthine disorder, vertigo, migraine**
33
Key mechanism of Warfarin (coumarin compounds)
**Vitamin K antagonist** Vitamin K is used to synthesis coagulation factors II (prothrombin), VII, IX, and X
34
Can Warfarin be used in pregnancy?
No because it crosses the placenta
35
Does Warfarin act immediately?
**No** because pool of circulating clotting factors needs to be depleted first. Synthesis of **new** factors is then inhibited. (takes 3-5 days to reach maximal effect)
36
What's the management of acute thromboembolic disorders?
LMWH (Low molecular weight heparin) plus warfarin, and then withdraw LMWH when warfarin is effective.
37
Patient advise for Warfarin
* Any signs of bleeding, including ecchymoses. * Contraindicated in pregnancy (fetal warfarin syndrome) * Avoid physical activities such as kick boxing * Don't \>\>\> green vegetables (vit K) * Avoid grapefruit juice, cranberry juice * Avoid major weight changes * Avoid aspirin, NSAIDs
38
Some common uses of Warfarin
Long-term treatment of **DVT** Patients with **AF** Patients with **artificial heart valves.**
39
Name three LMWHs
**enoxaparin** dalteparin tinzaparin
40
Key mechanism of heparin
**inactivates clotting factors** by **potentiating** the **activity** of an **endogenous anticoagulant** (antithrombin III)
41
Can Heparin be given orally?
No because heparin and related anticoagulants are not absorbed from the gut (large molecules) and so much be administered by IV.
42
What is antithrombin?
an endogenous anticoagulant (potent inhibitor of coagulation)
43
What is the principal component of fibrinolysis?
Enzyme plasmin (generated from inactive precursor plasminogen)2
44
What are the key adverse effects of Heparin?
Bleeding **thrombocytopenia** (hyperkalemia)
45
What's the antidote for warfarin-induced bleeding
Phytonadione (vitamin K1)
46
Clinicial uses for Warfarin
Long term management of DVT, AF, and artificial heart values.
47
What is the INR for recurrent embolization or **artificial heart valves**? What is the INR for warfarin (generally)
**3 - 4.5** 2-3
48
Name three **LMWH**
**enoxaparin** **dalteparin** **tinzaparin**
49
How does Dabigatran work?
**Direct thrombin inhibitor** (thrombin is used in the pathway of transforming fibrinogen to fibrin)
50
How does LMWH compare to unfractionated heparin in it's modus operandi?
Primarily deactive factor X
51
What's the **advantages of LMWH** compared to standard heparin?
can be administered **subcutaneously**. more **predictable** anticoagulation activity (aPTT monitoring not required)
52
What is HIT?
Heparin-induced-thrombocytopenia
53
Tell me about HIT 1
occurs in **25%** of patients. Direct interaction between heparin and platelets, leading to **platelet aggregation**. Mild and **reversible**.
54
Tell me about HIT 2
less common, **more serious**. **Immunoglobulin** **mediated** platelet inactivation. **High risk** of thrombotic complications and mortality.
55
How does **Fondaparinux** work?
**_Indirect_ Factor Xa inhibitor** It s**electively binds to antithrombin** (an endogenous anticoagulant) which **inactivates Xa** resulting in a strong inhibition of thrombin generation and clot formation.
56
How Warfarin monitored?
**Prothrombin Time (PT)**
57
What does INR stand for?
International normalized ratio INR = (PT observed / PT control) PT = prothrombin time
58
What is the antidote to unfractionated heparin and LMWH?
**Protamine sulfate** (+ve charged protein than combines with -ve charged heparin) \*\* measure **aPTT** to monitor \*\*
59
How do you monitor (a) Heparin (b) Warfarin (c) Dabigatran
(a) Heparin - aPTT **(b) Warfarin - PT - Prothrombin Time (remember the INR equation for warfarin)** (c) Dabigatran - TT (thrombin clotting time)
60
What initiates the formation of platelets along the vascular wall?
**injury** and the expose of the blood to extravascular **_collagen_**.
61
What activates the **intrinsic pathway**?
surface contact with a **foreign body** or **extravascular tissue** (i.e. collagen)
62
What activates the **extrinsic pathway** in the coagulation cascade?
a **complex tissue factor** called **thromboplastin**.
63
Where does the intrinsic and extrinsic pathways converge?
**Factor X -** major rate-limiting step
64
What does the activation of **factor X** lead to?
the formation of **Thrombin**
65
What three factors combined often lead to thrombic changes?
* **sluggish blood flow** * inflammation * **abnormalities in vascular endothelium**
66
What's the difference between arterial thrombi and venous thrombi?
**arterial thrombi** (white); more **platelet** aggrevation driven **venous thrombi** (red); more **coagulation** driven
67
**Aspirin**; clinical usages and action as an antiplatelet drug
**Acute coronary syndrome** **Thrombic strokes; acute and _prophylaxis_** **shown to prevent MI with _angina_.** Artificial heart valves, percutaneous coronary angioplasty. ACTION: inhibits the synthesis of **prostaglandins** from **arachidonic acid.**
68
What's the most important **prostaglandin** affecting platelet aggregation?
**prostacyclin** and **TXA2** (prostaglandin I2 (PGI2) Aspirin irreversibly inhibits cyclooxygenase; enzyme that catalyzes TXA2 synthesis.
69
Adverse effects of **aspirin**
**GI bleeding** **hypoprothrombinaemia**; therefore increased bleeding risks
70
When is clopidogrel indicated?
* px who can't tolerate aspirin * used in **COMBINATION** with aspirin for **_ACS_**
71
When are the representative drugs **steptokinase, alteplase** indicated?
intravenously to degrade thrombi in px with **MI, thromvotic stroke, PE** Primary means of restoring coronary blood flow if angioplasty facilities not available.
72
Adverse reactions with aspirin?
GI irritation, bleeding, hypersensitivity reactions, tinnitus
73
Adverse reactions to **streptokinase**
bleeding, hypersensitivity reactions, and reperfusion arrhymias (of interest) **anaphylactic shock** can occur with streptokinase, therefore cannot be used repeatedly on same patient.
74
what is **t-PA** and give an example drug
**Alteplase** drugs that are 'recombinant forms of human tissue plasminogen activator' **tissue-Plasminogen Activator**
75
How do Rivaro**_xa_**ban, Api**_xa_**ban, Edo**_xa_**ban work?
Direct Factor **_Xa_** inhibitor
76
How does **_D_**agiba**_t_**ran work?
**_D_**irect **_t_**hrombin inhibitor.
77
What's best for arterial thrombosis? Anticoagulants or antiplatelets?
Antiplatelets
78
Some advantages of NOACs/ DOACs
* few interactions with food/ drugs * predictable anticoagulant effect * no need for routine monitoring
79
Which pathway does Warfarin affect?
Both intrinsic and extrinsic
80
MOA of **Heparin**
binds to body's **own anticoagulant (antithrombin III)** This complex inhibits factor **Xa** (and other factors)
81
What is **Dipyridamole**? What is it indicated for?
**Dipyridamole** a coronary vasodilator and a relatively weak antiplatelet drug. **Dipyridamole** is used in **COMBO with aspirin** to prevent ischaemic stroke in px with history of thrombotic stroke, and persons experiencing TIAs.
82
What is Dipyridamole?
Dipyridamole is an **antiplatelet** medication that also has **vasodilating properties** that can make it **unsuitable** for use in those with severe coronary artery disease, unstable angina, recent myocardial infarction. Can be combined with **aspirin** as an option to prevent occlusive vascular events in patients who have had a **TIA**, or **ischaemic stroke**.
83
84
What kind of drug is Salbutamol?
Acts on the Beta 2 adrenergic receptors in the smooth muscle. It is a Beta 2 agonist drug.
85
What other drug (not salbutamol) is commonly used to treat asthma?
Ipratropium Bromide
86
What kind of drug is Ipratropium Bromide?
anti cholinergic bronchodilator
87
What group of drugs do respiratory consultants use for the management of asthma (2)? Name two.
Xanthines * aminophylline * theophyline Corticosteroids
88
How quickly does Salbutamol act, and how long does it last for?
2-5 mins about two hours
89
What's the typical dose of prednisolone for an acute asthma attack?
40-60mg orally or IV hydrocortisone 100mg if oral tablets not tolerated.
90
A common side effect from Salbutamol
tachycardia
91
What kind of neb would you use for an acute asthma attack (and dose)
**5mg** Salbutamol via O2 driven Nebuliser
92
What could you mix with Salbutamol for an acute asthma attack (and dose)?
ipratropium bromide 500ug (micrograms)
93
If usual meds are ineffective for acute asthma attack, what is worth trying?
magnesium sulphate 2g over 20 minutes via 200ml saline (mark saline bag with time)
94
What drugs can trigger an asthma attack?
B-Blockers NSAIDS
95
What is Cromolyn sodium and how does it work?
**Mast cell stabilizer** Stabilizes the plasma membrane of **mast cells** and **eosinophils** to prevent the release of histamine, leukotrienes, and other inflammatory mediators. (works by **blocking flux of Calcium** into the cells).
96
How are corticosteroids used to manage asthma?
Used on a long-term basis to **prevent asthmatic attacks**, rather than to treat acute bronchospasm.
97
Some examples of steroid inhalers (4)
**Beclomethasone** Budesonide **Fluticasone** Triamcinolone
98
Why is it not advisable to give **steroid inhalers** to children?
Possibly suppress **growth**. (another possible side effect; **oral thrush** from excessive steroid deposition in the mouth)
99
What are the **three** groups of bronchodilators?
**selective B2-adrenoceptor agonists** **muscarinic receptor antagonists** **theophylline** - all relax bronchial smooth muscle, but only **B2 agonists** are used in **acute** asthmatic attacks.
100
When are muscarinic antagonists indicated?
for **COPD** patients more than asthma patients.
101
When are theophyllines used?
**long-term basis to prevent bronchoconstriction** (with asthma or emphysema)
102
What are **Salmeterol** and **Formoterol** examples of, and when would they be prescribed?
**Long-acting B2-receptor agonists (LABA),** given twice daily by inhalation for the l**ong-term treatment** of asthma and emphysema. Particularly useful in preventing **nocturnal asthmatic attacks.**
103
How do Salmeterol and Formoterol work?
They inhibit the l**ate phase of allergen-induced bronchoconstriction.** (occurs after the bronchodilating effects of shorter-acting drugs have dissipated).
104
What type of drugs are Ipratropium and Tiotropium?
Muscarinic receptor antagonists (NB. Ipratroprium is a derivative of **atropine**).
105
Why would you use Ipratropium or Tiotropium in the management of COPD? (chronic bronchitis + emphysema)
Bronchodilating effect of ipratroprium is slower to develop than that of a B2-agonist, **_but it lasts longer._**
106
What is Advair (brand)?
**Fluticasone** (corticosteroid) **Salmeterol** (long-acting B2-receptor agonist)
107
What is **Symbicort**?
**Budesonide** (corticosteroid) **Formoterol** ( long acting B2 receptor agonist)
108
What is **Montelukast** an example of, and what is its mechanism?
**Leukotriene receptor antagonist** They have a structure similar to cysteinyl leukotrienes, and they **compete** with these substances for the **CysLT1 receptor.**
109
What is the clinical use of **Montelukast** and **Zafirlukast**?
Effective with patients with **allergic asthma**, including **aspirin-sensitive asthma,** and they maybe used to prevent **exercised-induced asthma** when taken at least two hours before the event. Effects of this drug are **accumulative**. Benefit **children** more than adults.
110
Ipratropium is typically a less effective B2-agonist in asthmatic patients, so why is it used in moderate to severe asthma?
Because it has a greater bronchodilating effect when used synergically with another B2 agonist in moderate to severe asthmatics.
111
How do the anticholinergic **muscarinic** receptor antagonists work? *(tiotropium and ipratropium)*
They block the bronchoconstricting effect of the vagal nerve (parasympathetic)
112
What are the adverse effects of **Leukotriene receptor antagonists** (eg. Montelukast)
Small number of patients can get **hypersensitivity** reactions. Rare cases of **liver injury**. NB\> this group of drugs is highly bound to plasma proteins (\>99%) and are extensively metabolized by hepatic cytochrome P450 enzymes.
113
What is Salmeterol?
Long-acting B2-receptor agonist
114
What is Formoterol?
Long-acting B2​-receptor agonist
115
What is Advair?
Fluticasone and Salmeterol
116
What is Symbicort?
Budesonide and Formoterol
117
What the the LABAs Salmeterol and Formoterol good for treating?
Late phase of allergen-induced bronchoconstriction, therefore useful at preventing nocturnal asthmatic attacks.
118
What is Combivent?
Albuterol and ipratropium (used to treat COPD).
119
Which drug lasts for 24 hours and is first -line treatment for COPD?
Tiotropium
120
What is a side effect of tiotropium and ipratropium?
dry mouth
121
Which drugs can inact with \> therapeutic range of theophylline
Cimetidine erthromycin fluoroquinolone, isoniazid and verapamil.
122
What is Omalizumab?
IgE antagonist given subcutaneously every 2-4 weeks in combination with inhaled corticosteroid therapy. (however this drug can cause allergic reactions)
123
Whats the MOA for theophylline?
acts at CNS and cellular level. Multiple actions on cell types and receptors.
124
What is theophylline used for?
COPD (20%\> in FEV1)
125
theophylline helps with COPD; in which ways?
**\>20% FEV1** \> diaphragmatic contactility **\> central respiratory drive** \> mucociliary clearance **\< inflammation** (used when COPD not controlled)
126
What is albuterol?
**Short acting inhaled B2 -agonist** (also levalbuterol)
127
What category are ipratropium and tiotropium and what are they primarily used for?
Muscarinic receptor antagonists Primarily used to treat COPD
128
What's the management for mild, persistent asthma?
Corticosteroid inhaler | (may be fluticasone or budesonide)
129
Why would you add a LABA?
If inhaled corticosteroid therapy is insufficient.
130
What's the advantage of B2 -agonists over nonselective B-receptor agonists?
They relax bronchial smooth muscle without producing so much tachycardia. HOWEVER; higher doses can activate cardiac B1-receptors and cause tachycardia.
131
What are the potential side effects of all B2-agonists?
tachycardia tremor nervousness
132
What is an adrenergic agonist?
An adrenergic agonist is a drug that stimulates a response from the adrenergic receptors.
133
What is the problem with B-adrenoceptor agonists and diabetes?
They stimulate **glycogenolysis** and thus can cause **hyperglycaemia**.
134
MOA of Cromolyn Sodium
Stabilize the plasma membrane of mast cells and eosinophils - mast cell stabilizer
135
Indications of Cromolyn Sodium
Prophylactic use. Indicated for exercise-induced asthma.
136
What's the use of LABAs?
Long-term treatment of **asthma** and **emphysema**. Particularly useful for preventing **nocturnal asthmatic attacks.** Salmeterol and Formoterol inhibit the **late phase** of allergen-induced bronchoconstriction.
137
Two examples of LABA
**salmeterol** and **formoterol**
138
What is Advair?
**_Advair: Fluticasone and Salmeterol_**
139
What is symbicort?
**_Symbicort: Budesonide and Formoterol_**
140
MOA of theophylline
Acts at the **CNS level** Also cellular level; blocks adenosine receptors, etc. Drug is bronchodilating, anti-inflammatory, and immunosuppressant.
141
Indications fo theophylline
**Long term use is associated with 20% increase in FEV1.** Reduces dyspnea, increases diaphragmatic contractility. Increases central respiratory drive. Increases muociliary clearance, reduces inflammation. **Used to treat COPD that isn’t controlled by B2 agonist and tiotropium.**
142
Theophyline fo asthma?
Usage is declining. Use if other drugs not working.
143
Drug interactions of theophylline
**Cimetidine** and **erythromycin** inhibit CYPP1A2 and increase theophylline plasma concentrations. Significant when drug is high in therapeutic range. Also **fluoroquinolone**, **isoniazid** and **verapamil**.
144
If serum level of theophylline is too high, then....
* 25mg/L ; **seizures and serious arrhythmias.**
145
What is Montelukast?
**Leukotriene receptor antagonis**t (they compete for the same leukotriene receptors)
146
Indications of Montelukast?
**Allergic asthma** (including aspirin-sensitive asthma) Prevention of **exercise-induced asthma** (take two hours before) **Accumulative** effect. Benefits **_children_** more and adults. Alternative for those not wishing to take steroids (although not so effective). Not as **effective as LABA as add-on to corticosteroids**, but may be safer.
147
Montelukast adverse effects?
use P450 pathway Occasionally hypersensitivity reactions. Rare – liver injury.
148
Side effects of B2 agonists
Tachycardia, tremor, nervousness
149
What do B1 agonists do?
stimulate cardiac muscle; increasing **rate** (chronotropic) and **strength** (inotropic), and **conductivity** (dromotropic)
150
Why are the anticholinergics **Ipratropium and tiotropium** used in **COPD**?
the bronchodilating effects of ipratropium is slower to develop than that of a B2-agonist, **but it lasts longer.** Improves quality of life in patients with moderate-severe COPD. Tiotropium; first-line treatment for patients with mild to severe COPD.