Pharmacology

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Pharmacology

• Units V VI

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Drugs for Diabetes Mellitus

• Type I destruction of beta cells, eventually no
  insulin production
• Type II usually begins in middle age - usually
  goes along with obesity insulin resistance,
  altered secretion

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Complications

• Short-term
• Hyperglycemia, hypoglycemia
• Ketoacidosis

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Complications

• Long-term
• Disruptions in blood flow
• Strict control of blood sugar may help prevent
• Cardiovascular complications
• Microvascular disease blood flow to
  microvascular lowered, kidney, blindness

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Complications

• Retinopathy
• Nephropathy renal disease primary cause of
  morbidity and mortality
• Neuropathy nerve damage
• Amputations
• Impotence
• Gastroparesis

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How do we diagnose?

• FBS
• Casual plasma glucose test
• GTT

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Type I treatment

• Monitor tight control of blood sugar
• Insulin
• Diet
• Exercise

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Type II treatment

• Control blood sugar
• Diet
• Exercise
• Oral hypoglycemic agents and/or insulin used as
  adjuncts

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Why do we need insulin?

• Actions are anabolic
• Conservation of energy and build up of energy
  stores
• Because of insulin (mostly) glucose converted
  into glycogen, amino acids to proteins, fatty
  acids into triglycerides

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Insulin deficiency

• Breakdown of complex molecules into simple stuff
• ketoacidosis

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Types of insulin

• natural insulin and four modified insulins
• Regular (Natural) unmodified, clear solution,
  generally rapid acting with shorter duration
• Only one that can be given IV

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• Lispro (Humalog) newer more rapid acting
  effects 5-15 minutes
• Usually given right before meals
• Only by prescription

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• NPH insulin regular mixed with protamine (large
  protein) delays absorption
• Longer acting

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• Lente mixed with zinc longer acting
  Ultra-lente longest acting
• U-100 and U-500 (available for patients with
  severe insulin resistance)

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Administration

• Given subcutaneously would be inactivated
  quickly if taken orally
• Only regular given IV if needed
• Sites upper arms, thighs, abdomen
• Make sure insulins are compatible when mixing

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Other methods of delivery

• Jet injectors
• Pen injectors
• Portable insulin pumps
• Implantable pumps
• Intranasal insulin

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Dosing schedule

• Conventional 2/3 given in am and remainder in
  evening long acting with shorter acting (lack
  of tight control)
• Intensive conventional therapy regular before
  each meal and ultra-lente in evening (tighter
  control)
• Continuous subcutaneous insulin infusion
  regular insulin (tight glucose control)

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Adverse effects

• Hypoglycemia must be treated rapidly
• Lipodystrophies
• Allergic reactions

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Oral hypoglycemics

• Sulfonylureas Orinase stimulates release of
  insulin by pancreas
• 2-3 times per day
• Adverse effects include hypoglycemia,
  cardiovascular toxicity?

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meglitinides

• Prandin
• Newer stimulates release of insulin from
  pancreas
• Must eat within 30 minutes of taking
• Short half-life

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Biguanides

• Metformin (glucophage) decreases glucose
  production in liver
• GI disturbances
• Must not be used in patients with renal disease,
  liver disease (lactic acidosis)

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Alpha-glucosidase inhibitors

• Acarbose delays absorption of dietary
  carbohydrates (by inhibiting a breakdown enzyme
  in the intestine)
• GI disturbances, liver dysfunction

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Thiazolidinediones

• Glitazones - increases ability of target cells
  to respond to insulin
• Troglitazone off market
• Avandia - safer

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Thyroid disorders

• T3 and T4 produced by thyroid gland
• Metabolism, cardiac function, growth and
  development
• T3 more potent
• Stimulation of energy use, stimulation of the
  heart, promote growth and development

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• Negative feedback from hypothalamus and anterior
  pituitary

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Hypothyroidism

• Signs and symptoms
• Lifelong treatment with thyroid replacement
• Levothyroxine (T4) orally, daily, 7 day half
  life

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Hyperthyroidism

• Graves disease and toxic nodular goiter
• Signs and symptoms
• Surgical removal of thyroid tissue
• Radioactive iodine
• Suppression of thyroid hormone synthesis with
  antithyroid drugs

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Drugs for hypothyroidism

• (PTU) Propylthiouracil inhibits hormone
  synthesis
• Short half-life, may take 1-2 weeks for effective
  therapy
• Agranulocytosis, hypothyroidism
• Methimazole

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• Radioactive iodine destroy thyroid tissue
• Iodide products Lugols solution high
  concentration produces suppression
• Propranolol

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Drugs for Asthma

• Inflammatory disorder of airway chronic
  p.824 process
• Airway inflammation edema, mucus plugging,
  smooth muscle hypertrophy, bronchoconstriction

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Glucocorticoids

• Inhalation, oral, IV
• Suppress inflammation, suppress release of
  inflammatory mediators, and inflammatory cell
  activity and decrease airway edema
• Inhaled first-line for asthma, daily basis

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• Oral glucocorticoids taken by patients with
  severe asthma
• Should be taken for brief periods

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Adverse effects

• Inhaled oralpharyngeal candidiasis
• Patients should gargle and use spacer (always) to
  prevent drug deposition in the oropharynx
• Oral glucocorticoids adrenal suppression,
  hyperglycemia, PUD, osteoporosis,suppression of
  growth

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Cromolyn

• Suppresses inflammation suppresses release of
  histamine etc.
• Administered by inhalation, give routinely
• Safest

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Beta2 adrenergic agonists

• For acute bronchospasm and exercise-induced
  bronchospasm
• Produce bronchodilation, more selective than
  epinephrine
• Inhaled or orally oral long acting

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Adverse effects

• Tachycardia, tremor, angina
• Albuterol and terbutaline oral agents

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Methylxanthines

• Theophylline CNS excitation and bronchodilation
• Taken po
• Narrow therapeutic range
• 5-15mcg/ml
• NV, diarrhea, restlessness

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Atrovent

• Ipratropium bronchospasm associated with COPD
• Muscarinic antagonist
• Promotes bronchodilation
• Can be given in combination with albuterol
  (Combivent)

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Drugs for Allergic Rhinitis, cough, colds

• Oral antihistamines relieve sneezing, runny
  nose, nasal itching
• Does not relieve nasal congestion
• Better to take prophylactically
• Sedation with first-line (benadryl)

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Intranasal glucocorticoids

• Anti-inflammatory effects relieves most all
  symptoms, even congestion
• Side effects mild if at all
• Make take a while to work 1-3 weeks depending

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Intranasal Cromolyn sodium

• Suppresses inflammation suppresses release of
  histamine, other inflammatory mediators from mast
  cells
• Delay of effectiveness
• Minimal side effects

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Sympathomimetics

• Decongestants
• Vasoconstriction, nasal blood vessels
• Relieve nasal stuffiness
• Oral or topical
• May have rebound congestion, CNS stimulation,
  cardiovascular effects, abuse

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Drugs for cough

• Antitussives suppress cough
• Opioid and nonopioid antitussives

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codeine

• Most effective elevates cough threshold
• Schedule II narcotic usually given in small
  doses though (mixtures are Schedule V)
• 10-20 mg orally
• Rarely given to children

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Nonopioid antitussives

• Dextromethorphan
• Acts within CNS, no abuse potential
• Nonprescription
• Diphenhydramine
• Tessalon local anesthetic

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Expectorants and mucolytics

• Expectorants stimulates flow of respiratory
  tract secretions guaifenesin
• Mucolytic makes mucus more watery cough more
  productive

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