Antidiabetics And Respiratory Drugs Flashcards
Asthma,cough,bronchitis,COPD
Aim of treatment of these conditions is to?-
Non productive cough is also called an irritative cough and coughs can be caused by obstruction true or false
Function of expectorant
reduce airway inflammation and bronchospams or bronchoconstriction
True
Enable the clogged airways to clear by reducing viscosity of mucus so it can easily flow or sometimes increase water content of mucus so it can easily flow
Drugs used in management of respiratory disorders
Drugs used in treating asthma
What are the classes of bronchodilators
How best to use these drugs to treat asthma is complex. A guideline on the management of asthma (BTS/SIGN, 2012) specifies five therapeutic steps for adults and chil- dren with chronic asthma. Very mild disease may be con- trolled with short-acting bronchodilator (salbutamol or terbutaline) alone (step 1), but if patients need this more than once a day, a regular inhaled corticosteroid should be added (step 2). If the asthma remains uncontrolled, step 3 is to add a long-acting bronchodilator (salmeterol or formoterol); this minimises the need for increased doses of inhaled corticosteroid. Theophylline and leuko- triene antagonists, such as montelukast, also exert a corticosteroid-sparing effect, but this is less reliable. One or other is added (step 4) for patients who remain symp- tomatic and/or the dose of inhaled corticosteroid increased to the maximum recommended. Step 5 is addition of a regular oral corticosteroid (e.g. prednisolone). True or false
Beta agonists-Beta 2 receptors found on the lungs open up airways (bronchodilators)
Glucocorticoids to control
inflammation (corticosteroids)
Leukotriene inhibitors
Antimuscarinics(main compound used as a bronchodilator is ipra- tropium. It is seldom used on a regular basis in asthma but can be useful for cough caused by irritant stimuli in such patients.
Ipratropium is a quaternary derivative of atropine and also nitrogen
Antihistamine (H1receptors)
: bronchodilators and anti-inflammatory agents.(glucocorticoids)
B2 adrenoreceptor agonists
Methylxanthines
Antimuscarinics (M3 receptor antagonist)
Leukotriene modifiers
sympa activation causes what in respiratory system (mechanism of action of beta 2 adrenoreceptor agonists)
Para activation causes what?
a glucocorticoid can be combined with a bronchodilator true or false
beta 2 adrenoceptors are activated to dilate bronchioles and relaxation of airway smooth muscle ,inhibition of mediator release from mast cells by preventing the degranulation of the mast cells cuz Degranulation of mast cells causes release of cytokines which will cause bronchoconstriction and cause inflammation
Increase Clearing of mucus (mucocilliary clearance)
causes increased secretions
True
Drugs for cough and give examples
Surfactants are used to treat COPd true or false and give two examples
Side effects of antitussives are constipation true or false
Leukolytics: break down of components in mucus
Antitussives :cough suppressants such as codeine ,dextromethorphan,pholcodine which are both opioid analgesics
Demulcents :soothe the airways.sometimes they contain an antiseptic (losenges
Expectorant :example guaifenesin
Basal decongestants
Anti fibrotics(used in cystic fibrosis)
beractant and poractant alpha (surfactant examples)
What are Bronchodilators
Name the types of Beta 2 agonists used in asthma
With examples
Tho adrenaline has effect on it we don’t use adrenaline
Why?
Give an example of methylxanthines and their mechanism of action
When are they given as injection
What are the side effects
Usually how are they given
They have A narrow therapeutic window and
Have positive chronotropic and inotropic effect on heart
True or false
Which drugs increase the half life of theophylline and which decrease it
You can give a beta 2 agonists with an antimuscarinic why?
Intravenously theophyllineis given (as aminophylline, a combination of theophylline with ethylenediamine to increase its solubility in water) in acute severe asthma true or false
Theophylline is given in addition to steroids true or false
Agents that give short term relief from bronchoconstriction by relaxing the airways smooth muscles
Long acting:tabeterol
Short acting:salbutamol and terbutaline
Terbutaline prodrug is bambuterol
SHORT-ACTING b2 ADRENERGIC AGONISTS Albuterol Levalbuterol LONG-ACTING b2 ADRENERGIC AGONISTS Arformoterol BROVANA Formoterol FORADIL, PERFOROMIST Indacaterol ARCAPTA Salmeterol Adrenaline is non selective cause it has effects on the other adrenoreceptors So while causing the dilation you’ll be causing other effects
Antimuscarinics that act as bronchodilators and acting against airway obstruction in asthma cuz activation of para leads to construction of airways
Only quartenary ammonium derivatives that are used ;ipratropium bromide
Side effects: dry mouth(cuz of prevention of secretion),prevents urination by causing urinary retention
Theophylline
They cause relaxation of bronchial smooth muscles by inhibition of phosphodiesterase enzyme4 and they inhibit adenosine which is an endogenous bronchoconstrictor and has some anti inflammatory properties
It is not first line treatment cuz it has plenty effects. Given as injection only in emergencies as aminophylline
Administered orally
Activate adenylyl cyclase causing increase CAMp causing bronchodilator
Phosphodiesterase enzyme breaks down CAMp
Inhibit adenosine- potent vasoconstrictor
Side effects:tachycardia,tremors,tachyarrythmias
Stimulation of CNS,convulsions ,seizures,can interact w other drugs cuz it’s also metabolized by CYP450,cardiac dysrhythmia
True
g. some antibiotics) increase the half-life of theophylline, others (e.g. anticonvulsants) decrease it.
Cuz they act differently
Beta 2 is acting on its receptor
Antimuscarnic is acting on M3 receptor
So they’re acting on two different receptors to cause bronchodilation
What are the classes of drugs used for their anti inflammatory effects on asthma ,their mechanism of action and examples
Give three examples of Corticosteroids usually used in asthma
How are they given
When are they given orally
What are the side effects of glucocorticoids
Patients with acute exacerbations of asthma may require intravenous hydrocortisone and oral prednisolone. True or false
What are the type of antihistamines with examples
Glucocorticoids or corticosteroids : • The mechanism of action involves decreased
formation of cytokines, particularly those generated by Th2 lymphocytes, decreased activation of eosinophils and other inflammatory cells.
Mast cell stabilizers : Drugs that prevent degranulation of mast cells: they stabilize mast cells examples: Cromoglicate and nedocromil,cromolyn
beclometasone, budeso- nide, fluticasone, mometasone and ciclesonide,These are given by inhalation with a metered-dose or dry powder inhaler, the full effect on bronchial hyper-responsiveness being attained only after weeks or months of therapy. Oral glucocorticoids .are reserved for patients with the severest disease.
Sometimes combine w beta 2 agonists in an inhaler
Prenisolone-side effects
Lead to Cushing’s syndrome
Can affect metabolism
It is withdrawn slowly cuz it has withdrawal effects
Sedating antihistamines example piritine
Non sedating antihistamine example
Asthma
How it occurs
What is it
Antimuscarinic bronchodilators should be used w caution in patients BPH why?
Acute severe asthma
A medical emergency
Not easily reversed true or false
Increased airways smooth muscle size causing constriction of airways
Bronchial hyperreactivity
A chronic inflammatory condition in which there is recurrent reversible airway obstruction
Bronchodilators (plus all four classes)
Glucocorticoids
Is used in oral form and inhaler
The aerosol is directed to the site of action cuz if given systemically it’ll keep long true or false
What is an aerosol
Tolerance develops when a beta 2 agonists is used for a long time that’s why it’s better to use SABA regularly and LABA in emergencies true or false
True
Contents are compressed in the container so when sprayed they come out in a mist or fog
They are formulated with a propellant
True
Leukotriene modifiers
Mechanism of action
Leukotriene modifiers don’t affect underlying airway inflammatory disorders
Cysteinyl leukotriene receptor antagonists (e.g. montelukast) are third-line drugs for asthma. asthma. Theycompete with cysteinyl leukotrienes at CysLT1 receptors and are used mainly as add-on therapy to inhaled
corticosteroids and long-acting β2 agonists
True or false
Lipooxygenase pathway isn’t good for asthma or respiratory disorders
They prevent the pathway from happening Inhibit enzyme or block receptor Zinotin-lipooxygenase inhibitor Leukotriene antagonist-montelukast The lukasts are taken by mouth, in combination with an inhaled corticosteroid.
It’s a mechanism so if you’re taking these drugs and the products have already been formed it can’t have effect on the products that have already been formed
True
Mast cell stabilizers Mechanism of action Give examples Which other class of drugs Effect of corticosteroids are not immediate so they’re not used as relievers but controllers true or false
Side effects of corticosteroids
Prevent mast cells from degranulation
Immunoglobulins and immunosuppressant
Occur due to prolonged use of Cushing’s syndrome:muscle wasting ,immunosupression,cataract,moon face,hypertension,buffalo eyes
Corticosteroids Are not started and stopped abruptly
What happens to the body when we are hyperglycemic
Difference between diabetes and hyperglycemia
Increased blood glucose causes increased free fatty acids,insulin resistance,decreased insulin all leading to oxidative stress
Oxidative stress causes decreased nitric oxide ,increased endothelin-1, increased angiotensin II all leading to vasoconstriction causing hypertension,vascular smooth muscle cell growth
Oxidative stress also causes Decreased Nitric Oxide,increased Angiotensin ll,Activation of activator protein -l All causing Inflammation: Release of chemokines Release of cytokines Expression of cellular adhesion molecules
Oxidative stress also causes reduced Nitric oxide,increased Tissue factor,increased Plasminogen Activator,decreased Prostacyclin Leading to Thrombosis: Hyper coagulation Platelet Activation Decreased Fibrinolysis
Diabetes is the disease,hyper is the symptom
Insulin counter glucose to keep body in a balanced way. It’s produced by beta cells of pancreas. True or false
How is diabetes diagnosed
What is HbA1C
What is the difference between type 1 and type 2 diabetes
What are the complications of type 1 diabetes
Oral anti diabetic drugs are not effective in type 1 but are given in type 2
True
Oral glucose tolerance test
What is a HbA1c?
It is a test that allows healthcare providers to see how diabetics have managed their blood glucose level over the last 2-3 months
Type 1 Lack of insulin production OR Production of defective insulin Affected patients need exogenous insulin Insulin dependent diabetes
Type 2
Most common type
Caused by insulin deficiency and insulin resistance
Many tissues are resistant to insulin
◦Reduced number insulin receptors
◦Insulin receptors less responsive
◦These people respond to oral hypoglycemics
Complications
◦Diabetic ketoacidosis (DKA)
◦Hyperosmolar nonketotic syndrome
Cuz there is no insulin being produced so there’s no beta cell function for the orals to act on. The orals counter hyperglycemia which has increased due to insulin resistance or low levels of insulin being produced by causing increased secretion of insulin from beta cells
Therapy in type 2 is supplemented w insulin . Especially in complications or when the orals aren’t working true or false
Signs and symptoms of type 1 and type 2 diabetes
When put on the Thiazolidinediones patients need to be put on liver function test to monitor the liver cuz it can cause damage. True or false
True
Type 1 Weight loss Fatigue Rapid onset Increased frequency of infection
Type 2 Sedimentary lifestyle Familial tendency History of high bp Fatigue and low energy Obese Recurrent infections Polyuria Polydipsia FBs-less than 126mg/dl
What are the Classes of oral hypoglycemics
Sulfonylureas (oldest)
● Meglitinides
● Biguanide-metformin
● Thiazolidinediones
When the agents stimulate production of insulin
It can cause hypoglycemia as a side effect
True or false
True
Metformin has to be taken a lot and that’s a disadvantage true or false
Metformin doesn’t deal with insulin directly that’s why you can combine a biguanide use and a sulfonylurea drug true or false
They’re not given directly w insulin so they don’t cause an increase in insulin secretion
True or false
True
True
True
Name five Comorbid conditions of type 2 diabetes
Several comorbid conditions
•metabolic syndrome OR insulin-resistance syndrome OR syndrome X
◦Obesity ◦Coronary artery disease ◦Dyslipidemia ◦Hypertension ◦Microalbuminemia (protein in the urine) ◦Enhanced conditions for embolic events (blood clots) ◦Insulin Resistance
What is gestational diabetes
What is given to prevent birth defects
In gestational diabetes 4% of all pregnancies
◦Must be reclassified if it persists 6 weeks post-delivery
◦Usually subsides after delivery
◦30% of patients may develop Type 2 DM within 10 to 15 years true or false
Hyperglycemia that develops during pregnancy
◦Insulin must be given to prevent birth defects
◦
What are the differences in treatment of type 1 and type 2 diabetes
When will insulin be given in type 2
Name five complications associated w diabetes Mellitus
Type 1
◦Exogenous insulin
◦Dietary control
•
Type 2 ◦Lifestyle changes •Dietary control •Weight reduction •Exercise ◦May require oral hypoglycemic therapy or exogenous insulin ◦
Insulin when oral hypoglycemic medications can no longer provide glycemic control
Cardiovascular disease, including hypertension o Peripheral vascular disease o Delayed healing o Visual defects, including blindness o Renal disease o Infection o Neuropathies o Impotence
Name three indications for oral hypoglycemics
Name three contraindications for oral hypoglycemics
They are used to lower blood sugar levels in patients that diet and exercise have failed.
The patient must have some pancreatic function left.
They can be used as a monotherapy or in conjunction with other oral hypoglycemics.
Known drug allergy
Active hypoglycemia
Usually not used during pregnancy subq insulins are used then.
Liver disease
Kidney disease
◦Depending on the metabolic pathways of the medication
Name three first generation and second generation sulfonylurea drugs
Which is commonly used?
Which patients can’t take sulfonylurea drugs else it’ll cause hemolytic anemia
What is the mechanism of sulfonylurea drugs
Name four the adverse effects of sulfonylurea drugs
First generation: ◦chlorpropamide ◦tolazamide ◦tolbutamide ◦ Second generation: ◦glimepiride ◦glipizide ◦glyburide
The second generation
G6PD patients
Patients with sulphuric allergies can’t take sulfonylurea
Stimulate insulin secretion from the beta cells of the pancreas, thus increasing insulin levels
Beta cell function must be present
Improve sensitivity to insulin in tissues
Result: lower blood glucose levels
Sulfonylureas ◦ Hypoglycemia ◦ hematologic effects ◦ nausea ◦ epigastric fullness ◦ heartburn ◦ many others
What is the difference between meglitinide and sulfonylurea drugs
Name some examples of meglitinide drugs
Mechanism of action
Name five adverse effects of this drug
Meglitinide doesn’t have sulphur in it so can be given to patients with sulphur allergies
Meglitinides
◦repaglinide (Prandin)
◦ nateglinide (Starlix)
Meglitinides
◦Action similar to sulfonylureas
◦Increase insulin secretion from the pancreas
Meglitinides ◦Headache ◦Hypoglycemic effects ◦Dizziness ◦Weight gain ◦Joint pain ◦Upper respiratory infection or flu-like symptoms
Biguanides can be given together with sulfonylurea drugs true or false
Give examples of this class of drugs
What is the mechanism of action
State five adverse effects
Biguanides do not cause hypoglycemia true or false
True
Biguanides
◦metformin (Glucophage)
Biguanides
◦Decrease production of glucose
◦Increase uptake of glucose by tissues
◦Does not increase insulin secretion from the pancreas (does not cause hypoglycemia)
Metformin
◦Primarily affects GI tract: abdominal bloating, nausea, cramping, diarrhea, feeling of fullness,May also cause metallic taste, reduced vitamin B12 levels,Lactic acidosis is rare but lethal if it occurs
True
Give some examples of Thiazolidinediones
These class of drugs are also known as?
What are the mechanisms of actions of these drugs
What are the adverse effects
Thiazolidinediones ◦pioglitazone ◦rosiglitazone ◦Also known as “glitazones” Thiazolidinediones ◦Decrease insulin resistance ◦“Insulin sensitizing drugs” ◦Increase glucose uptake and use in skeletal muscle ◦Inhibit glucose and triglyceride production in the liver
Adverse effects:
Moderate weight gain
Edema
◦Mild anemia
◦Hepatic toxicity—monitor liver function tests
Give some examples of Alpha-glucosidase Inhibitors
Mechanism of action and advert effects
Alpha-glucosidase inhibitors
◦acarbose (Precose)
◦miglitol (Glyset)
Alpha-glucosidase inhibitors
◦Reversibly inhibit the enzyme alpha-glucosidase in the small intestine
◦Result: delayed absorption of glucose
◦Must be taken with meals to prevent excessive postprandial blood glucose elevations (with the “first bite” of a meal)
Flatulence
◦ diarrhea
◦ abdominal pain
◦Do not cause hypoglycemia, hyperinsulinemia, or weight gain
Name the three classes of newer oral agents for diabetes as long as their examples each
What is the function of GLP-1,dipeptidil peptidase-4 enzyme
Insulin is given subcut and it should be rotated like given at different places not one place at the same time
Glucagon-like peptide-1 (GLP-1) agonists (in type 2 DM): increase pancreatic secretion of insulin. Eg. Exenatide, Liraglutid
Inhibitors of Dipeptidil peptidase-4 (DPP-4): prevent degradation of incretin GLP-1. eg. Sitagliptin, Vildagliptin
Inhibitors of reabsorption of glucose (SGLT2 inhibitors): eg. Canagliflozin, dapagliflozin
GLP-1:
Endogenous molecule which causes increased insulin production ,increased uptake of glucose . Demerit:very short acting
Dipeptidil peptidase-4 enzyme degrades the GLP-1 making it short acting
What is the mechanism of action of insulin
What are the goals of using insulin
Some Insulin is derived from porcine sources and new ones are human derived using recombinant DNA technologies true or false
What are the indications of insulin
What are the adverse effects
Substitute for & same effects as endogenous insulin
Restores the diabetic patient’s ability to:
◦Metabolize carbohydrates, fats, and proteins
◦Store glucose in the liver
◦Convert glycogen to fat stores
Goal: tight glucose control
◦To reduce the incidence of long-term complications
True
To treat both types of diabetes
Each patient requires careful customization of the dosing regimen for optimal glycemic control
Are all signs and symptoms of hypoglycemia including shock and death.
What are the types of human based insulin and give examples each of them
Which insulin product is given IV or even IM
How is Rapid acting given
How is isophane insulin given
Which insulin is Slower in onset and more prolonged duration than endogenous insulin
Rapid-Acting
◦Most rapid onset of action
◦Shorter duration
aspart (Novolog)
lispro (Humalog)
glulisine (Apidra)
Short acting :
regular insulin (Humulin R, Novolin R)
Onset 30 – 60 minutes
◦The only insulin product that can be given by IV bolus, IV infusion, or even IM
Intermediate-Acting
◦isophane insulin suspension (also called NPH) (Humulin N, Novolin N)
Lispro protamine suspension (Humalog 75/25, Novolog Mix 70/30)
insulin zinc suspension (Lente, Novolin L)
◦Cloudy appearance
◦
Combination insulin products:
NPH 70% and regular insulin 30% (Humulin 70/30, Novolin 70/30)
NPH 50% and regular insulin 50% (Humulin 50/50)
insulin lispro protamine suspension 75% and insulin lispro 25% (Humalog Mix 75/25)
Short acting
May be given SC or via continuous SC infusion
pump (but not IV)
isophane insulin suspension & insulin injection
(Humulin 50/50 , Humulin 70/30, Novolin 70-30)
Immediate acting insulin
What are the early and Late signs of hypoglycemia which is an adverse effect of insulin
Which level of blood glucose is abnormally low
Mild cases of hypo is treated by?
What’s re the general signs of hypo
Early
◦Confusion, irritability, tremor, sweating
•Later
◦Hypothermia, seizures
◦Coma and death will occur if not treated
<50 mg/dL
Mild cases can be treated with diet—higher intake of protein and lower intake of carbs—to prevent a rebound postprandial hypoglycemia
Tachycardia Irritability Restlessness Excessive hunger Diaphoresis Depression (TIRED)
What is DKA
What causes it
DKA is a sudden onset true or false
Factors of DKA
What are the symptoms of DKA
These are the results for DKA: Glucose >300 mg/dL pH <7.35 / Bicarbonate < 15 mEq/L Na – low / K+ > / Cr >1.5 mg/dL Blood & Urine Ketones - Positive true or false
State of hyperglycemia with ketosis
Usually results from infection, environment, or emotional stressor
◦As a result of lack of Insulin, breakdown:
◦Fat – free fatty acids in liver – ketone bodies – ketones in urine
◦Protein – to form new glucose / increased BUN
◦Glycogen to glucose (decrease use of glucose because of decreased insulin)
◦Osmotic diuresis
◦Dehydration / Electrolyte Imbalance
◦Hyperosmolality Hemoconcentration
◦Acidosis
◦Death
True
Factors: infection, stressors, inadequate insulin
Kussmaul respiration / fruity odor to breath, nausea, abdominal pain
Dehydration, electrolyte imbalance, polyuria, polydipsia, weight loss, dry skin, sunken eyes, soft eyeballs, lethargy, coma
True
Which drugs can damage the lung tissue
What are characteristics of asthma
amiodarone, methotrexate
inflammation of the airways • bronchial hyper-reactivity
• reversible airways obstruction.
Name some sedating (1st generation)and non sedating (2nd generation)anti histamines
generation H1 antihistamines, such as chlorpheni- ramine [klor-fen-IR-a-meen], diphenhydramine, hydroxyzine hye- DROX-ee-zeenand promethazine,
2nd generation Cetirizine. Desloratadine. Loratadine. Fexofenadine.
Give some examples of inhaled corticosteroids, LONG-ACTING b2 ADRENERGIC AGONIST/CORTICOSTEROID, LONG-ACTING ANTICHOLINERGIC
INHALED CORTICOSTEROIDS Beclomethasone Budesonide, Ciclesonide,, Fluticasone Mometasone Triamcinolone
LONG-ACTING b2 ADRENERGIC AGONIST/CORTICOSTEROID C Formoterol/budesonide Formoterol/mometasone Salmeterol/fluticasone Vilanterol/fluticasone
SHORT-ACTING
ANTICHOLINERGIC :Ipratropium
LONG-ACTING ANTICHOLINERGIC: Aclidinium bromide ,Tiotropium
Which leukotriene modifiers is a selective and specific inhibitor of 5-lipoxygen- ase, preventing the formation of both LTB4 and the cysteinyl leu- kotrienes.
Which leukotriene modifiers are selective antagonists of the cysteinyl leu- kotriene-1 receptor
Food impairs the absorption of zafirlukast. The drugs are metabolized extensively by the liver. Zileuton and its metabolites are excreted in urine, whereas zafirlukast, montelu- kast, and their metabolites undergo biliary excretion. True or false
Zileuton
Montelukast
Zafirlukast
The effects of corticosteroids are not intermediate so they’re used a preventers not relievers true or false
Theophylline is not soluble ,nor a first line treatment and can’t be given as an injection unless it’s given as aminophylline true or false
True
True
