Download DRUGS USE IN ENDOCRINE SYSTEM

DRUGS USE IN ENDOCRINE
SYSTEM
DRUGS USE IN
DIABETES MELLITUS
What is diabetes?
• Diabetes mellitus is a group of metabolic
diseases characterized by high blood
glucose levels (hyperglycemia), that result
from defects in insulin secretion, or action,
or both
• TYPE I DM
• TYPE II DM
TYPE I DM
• In type 1 diabetes (formerly called insulindependent diabetes or juvenile-onset
diabetes), more than 90% of the insulinproducing cells of the pancreas are
permanently destroyed.
• The pancreas, therefore, produces little or
no insulin.
• Treatment of choice will be insulin
TYPE II DM
• In type 2 diabetes (formerly called noninsulin-dependent diabetes or adult-onset
diabetes), the pancreas continues to
produce insulin but body develops
resistance to the effects of insulin, so there
is not enough insulin to meet the body's
needs
• Some times with age the production of
insulin not enough to meet the demand
• In type 2 can use insulin and other
antidiabetic drugs
INSULINS
• People with type 1 diabetes almost always
require insulin therapy, and many people
with type 2 diabetes also require insulin
with time when it becomes difficult to
control with oral antidiabetics
• Insulin is injected
• It currently cannot be taken by mouth
because insulin is destroyed in the
stomach since it’s a polypeptide hormone
• Insulin is injected under the skin into the
fat layer, usually in the arm, thigh, buttock
or abdominal wall ( subcutaneous)
• Small syringes with very thin needles
make the injections nearly painless (
usually 28 to 31 gauge needles)
• Insulin is available in three basic forms,
divided by speed of onset and duration of
action
Types of insulin
• Short acting or rapid acting or regular
insulin
• Intermediate acting insulin
• Long acting insulin
Short acting or rapid acting or
regular insulin
• Rapid-acting insulin, such as regular
insulin, is fast and short acting.
• Regular insulin reaches its maximum
activity in 2 to 4 hours and works for 6 to 8
hours.
• Lispro, aspart, and soluble insulins,
special types of regular insulin, are the
fastest of all, reaching maximum activity in
about 1 hour and working for 3 to 5 hours
• Rapid-acting insulin is often used by
people who take several daily injections
and is injected 15 to 20 minutes before
meals or just after eating
• Soluble insulin is the best insulin for
emergencies; it can give IV, IM and SC
Intermediate acting insulin
• Intermediate-acting insulin (such as zinc
suspension, lente, or isophane insulin
suspension) starts to work in 1 to 3 hours,
reaches its maximum activity in 6 to 10
hours, and works for 18 to 26 hours.
• This type of insulin may be used in the
morning to provide coverage for the first
part of the day or in the evening to provide
coverage during the night.
Long acting insulin
• Long-acting insulin (such as extended
zinc suspension, ultra-lente, or glargine)
has very little effect in the first few hours
but provides coverage for 20 to 36 hours
depending on which of these types is used
• Generally subcutaneous insulin cause few
problems like fat hypertrophy and allergic
reactions
• Allergic reactions are very rare at present
• Fat hypertrophy also minimize by rotating
the site
Insulin Storage
1. Never freeze. (Frozen insulin should be
thrown away.)
2. Never use insulin beyond the expiration
date
3. Never expose insulin to direct heat or light
4. Inspect insulin prior to each use. Any
insulin that has clumps or solid white
particles should not be used. Insulin that is
supposed to be clear should not have any
cloudy appearance.
5. Check storage guidelines specific to the
insulin formulation. This is usually in the
product package insert.
6. Insulin should be stored in a refrigerator
(not to be freezed)
7. When storing pre-filled insulin syringes,
store them with the needle pointing up
Oral hypoglycemic agents
Biguanides
Sulfonylureas
Meglitidines
Thiazolidinediones
Alpha-glucosidase inhibitors
SULPHONYLUREAS
• Act mainly by augmenting insulin secretion
and effective only when residual
pancreatic beta cell activity is present
• SE include GI disturbances, rarely
disturbances of liver functions
• CI include severe hepatic and renal
impairment, pregnancy and breast feeding
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Chlorpropamide
Long acting
Glibenclamide
Gliclazide – short acting
Glimepiride
Glipizide
Gliquidone
Tolbutamide – short acting
BIGUANIDES
• Metformin hydrochloride is the only
available biguanide
• It exerts its effect mainly by decreasing
gluconeogenesis and by increasing
peripheral utilisation of glucose
• Since it acts only in the presence of
endogenous insulin it is effective only if
there are some residual functioning
pancreatic islet cells
• Metformin is the drug of choice in
overweight patients since it causes
anorexia
• Other SE include nausea, vomiting,
diarrhea, abdominal pain
• CI in renal impairment, pregnancy and
breast feeding
Hypoglycemic attacks more
common with sulphonylureas
than with biguanides
Oral hypoglycemic agents
Meglitidines
modulates B cell insulin release by regulating potassium efflux through the
potassium channels
Oral hypoglycemic agents
Thiazolidinediones
enhance target tissue insulin sensitivity-
rosiglitazone,
pioglitazone
Their main action is to diminish insulin resistance by increasing glucose uptake
and metabolism in muscle and adipose tissues.
Can cause oedema as a SE
Alpha-glucosidase inhibitors
Acarbose and miglitol are competitive inhibitors of the intestinal
enzymes and modulate the digestion and absorption of starch
THYROID AND
ANTITHYROID DRUGS
Thyroid hormones
• Thyroid hormones are used for the
treatment of hypothyroidism
• Levothyroxin sodium (thyroxin sodium) is
the treatment of choice for maintenance
therapy
• Taking preferably in the morning
• SE-if taken more can cause
hyperthyroidism
Antithyroid drugs
• Antithyroid dugs are use for
hyperthyroidism
• Carbimazole
• Propylthiouracil
Carbimazole
• Carbimazole is an antithyroid agent that
decreases the uptake and concentration of
inorganic iodine by thyroid, reducing the
formation of thyroxine
• SE includes GI disturbances, rash,
arthralgia, alopecia, bone marrow
suppression ( if patient develop sore throat
it’s a sign of agranulocytosis which
immediately should report to the clinician)
• Propylthiouracil also same as carbimazole
CORTICOSTEROIDS
Corticosteroids
• Produced by the adrenal cortex
• Involved in stress response, immune
response and regulation of inflammation,
carbohydrate metabolism, protein
catabolism, blood electrolyte levels and
behavior.
Uses of Corticosteroids
• Use to treat a number of different disorders
especially inflammatory or immunologic disorders
• Arthritis
• Dermatitis
• Allergic reactions
• Asthma
• Hepatitis
• Lupus erythematosus
• Inflammatory bowel disease: ulcerative colitis and
Crohn’s disease
• Uveitis – inflammation of eye
Replacement therapy
• Indicated when the adrenal gland not
functioning properly or when the gland is
removed
• Usually use a combination of
hydrocortisone (glucocorticoid) and
fludrocortisone (mineralocortocoid) for
complete replacement
• Usually larger dose in the morning and
smaller dose in the evening
• Use as oral drugs on regular basis; but in
acute adrenal insufficiency hydrocortisone
is given intravenously
Side Effects
• Moon face, buffalo hump, obese trunk (love
handles), acne, hirsutism, weight gain
• Impaired healing or bruising
• CNS: nervousness, insomnia, depression,
aggravation of pre-existing mental disorders
• Musculoskeletal: long term use can cause
osteoporosis, muscle weakness and atrophy
• GI: peptic ulcer, increased appetite
• Cardiovascular: fluid retention
• Ocular: increased intraocular pressure, glaucoma,
cataracts
Moon Face
High-dose
corticosteroid therapy
produces a characteristic
“moon face” appearance.
Glucocorticoid therapy
• Mostly as antiinflammatory agents in
inflammation and allergies
• Prednisolone
• Betamethasone
• Cortisone acetate
• Deflazacort
• Dexamethazone
• Hydrocortisone
• Methylprednisolone
• Triamcinolone
• All these drugs contraindicated in systemic
infections
• Avoid live virus vaccines those who are
receiving immunosuppressive doses
SEX HORMONES
Female sex hormones
Male sex hormones
Female sex hormones
• Main indication is hormone replacement
therapy
• If long therapy of estrogen is required a
progesteron also should be added to
reduce the risk of hyperplasia of the
endometrium and possible transformation
to cancer
Hormone Replacement Therapy
• Helps to relive symptoms of menopause
such as such as hot flashes, vaginal
dryness, mood swings, sleep disorders,
and decreased sexual desire.
• Specially improve the conditions such as
osteoporosis and urinary incontinence
Complications
• Increase risk of deep vein thrombosis and
pulmonary embolism
• Increase risk of breast cancer when using
for more than 5 years
• Increase risk of endometrial cancer when
using estrogen alone
• Increase risk of stroke
• Does not prevent coronary heart disease
Estrogens
Side effects
• GI disturbances, weight changes, breast
enlargement and tenderness,
premenstrual like syndrome, sodium and
fliud retention, altered blood lipids,
cholestatic jaundice, rashes, changes in
libido, depression, headache, migraine,
dizziness, leg cramps
Contra indications
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Pregnancy
Oestrogen dependent cancer
History of breast cancer
Active thrombophlebitis
Angina, MI
Venous thromboembolism
Liver disease
Undiagnosed vaginal bleeding
Breast feeding
Untreated endometrial hyperplasia
Progestogens
• Other than hormone replacement therapy
use in oral contraception, to treat
endometriosis, recurrent miscarriages,
infertility, dysfunctional menstrual bleeding
Side effects
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Menstrual disturbances
Premenstrual like syndrome
Weight gain
Nausea
Headache, dizziness
Insomnia
Drowsiness
Depression
Fluid retention
• Urticaria, pruritus, rash and acne
• Hirsutism and alopecia
Contraindications
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Liver diseases
Arterial diseases
Genital or breast cancers
Undiagnosed vaginal bleeding
Porphyria
• Dydrogesterone
• Medroxyprogesterone acetate
• Norethisterone – use for postponement of
menstruation, 5mg tds starting 3 days
before anticipated onset (menstruation
occurs 2 to 3 days after stopping)
• Progesterone
Male Sex Hormones
• Use to treat androgen deficiency
• Testosterone and esters
• SE include prostate abnormalities,
prostate cancer, headache, depression, GI
bleeding, nausea, cholestatic jaundice,
hypertension, oedema, hypercalcaemia,
increase bone growth,
• Androgenic effects such as hirsutism,
male pattern baldness, acne, excessive
frequency and duration of penile erection,
precocious sexual development, virilism in
women
• CI in breast cancer in men, prostate
cancer, liver tumors, hypercalcaemia,
nephrosis, pregnancy and breast feeding
HYPOTHALAMIC AND
PITUITARY HORMONES
Anterior pituitary hormones
• ACTH
• Gonadotrophins
Chorionic gonadotrophin, HCG
Chorionic gonadotrophin
• In females, chorionic gonadotropin is used
to help conception occur
• Use in many women being treated with
clomiphene and other drugs such as
follitrophin and have not been able to
conceive yet.
• Chorionic gonadotropin is also used in in
vitro fertilization (IVF) programs.
• In males, LH and chorionic gonadotropin
stimulate the testes to produce male
hormones such as testosterone.
• Testosterone causes the enlargement of
the penis and testes and the growth of
pubic and underarm hair.
• It also increases the production of sperm
• SE include edema, headache, tiredness,
mood changes, gynaecomastia, local
reactions
• CI in androgen dependent tumors
• Use as SC or IM injections
Growth hormone
• Somatrophin – synthetic human GH
• Indicated in GH deficiency, Turner
syndrome, Prader – Willi syndrome
• SE include headache, papilloedema,
visual problems, nausea and vomiting
• CI in any evidence of tumor
• vasopressin and desmopressin
– Used in the treatment of diabetes insipidus
– Used in the treatment of various types of
bleeding, especially GI bleeding
– desmopressin is useful for:
• Hemophilia A
• Type I von Willebrand’s disease
Thank you…