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IUD
1. Intra Uterine Devices
Presented by:
Vrushali V . Sonawadekar.
1st YEAR M-PHARM
Department of Pharmaceutics
KLEU college of Pharmacy Belagavi.
2. ďś Introduction
ďContraception
ďAnatomy of uterus
ďMenstrual cycle
ďś Desirable features of intra vaginal DDS
ďś IUDâS
ďś Development of IUDâs
ďś Types of IUDâs
1) non medicated
2) medicated a) copper bearing IUD
b) hormone releasing IUD
CONTENTS
3. TERMSâŚ.
CONTRACEPTION: (def)
ď It is the method which results into temporary or permanent loss of
capability to reproduce or conceive a young one.
ď In simple words it is the opposite of conception.
ď There are 2 types of contraception: Temporary and permanent.
ď Temporary contraception: It is a method or lifestyle that ensures
reversible infertility for stipulated period of time depending on the
subject.
e.g. IUDâs, oral contraceptive pills, condoms etc
ď Permanent contraception: It is the method or technique adopted to
give life long acquired inability to reproduce, but it is not the loss of
sense or loss of sexual desire.
ď e.g. ovarectomy, uterectomy, vasectomy, etc.
5. ďŹ The uterus is a pear shaped, thick-walled, muscular organ suspended in
the anterior wall of pelvic cavity.
ďŹ In its normal state, it measures about 3 inches long and 2 inches wide.
ďŹ Fallopian tubes enter its upper portion, one on each side, and the lower
portion of the uterus projects into the vagina.
ďŹ The uterine cavity is normally triangular in shape and flattened anterio-
posteriorly.
6. The wall of the uterus consists of 3 layers:
1. Endometrium- Inner coat of the uterine wall and is a mucous
membrane. It consists of epithelium lining and connective tissue.
Epithelium consists of non-cornified stratified sqamous
epithelium, and lamina propria.
Squamous epithelium sub-divided into 4 layers:
Superficial - large, flat cells.
Intermediate â larger flatter nucleated cells
Parabasal â polyhedral cells
Monolayer â cuboidal basal cells closely apposed to basement
membrane.
Connective tissue consists of two types of arteries which supply
blood to the endometrium- straight arteries supply the deeper
layer; the coiled arteries supply the superficial layer.
7. 2. Myometrium- Thick, muscular middle layer made up of bundles of
interlaced, smooth muscle fibers emmbeded in connective tissue. It is
Sub-divided into 3 ill-defined, intertwining muscular layers
containing large blood vessels of uterine walls.
3. Peritoneum- External surface of the uterus, which is attached to the both
sides of the pelvic cavity by broad ligaments through which the
uterine arteries cross.
8. MENSTRUAL CYCLE
Human femaleâs fertility period, extends from puberty at
about 13 years to about 45-50 years. The menstrual cycle
consists of 3 phases:
ďŹ Follicular or proliferating phase
ďŹ Luteal or secretory phase
ďŹ Menstrual or bleeding phase
FOLLICULAR PHASE
1. It lasts for 14 days.
2. Follicle stimulating hormone (FSH) stimulates the growth of
ovarian follicle and maturation of the primary oocyte in this
follicle.
3. FSH stimulates the follicles to secrete estradiol which on attaining
a certain concentration in blood inhibits FSH secretion and
stimulates Leuteinising hormone (LH) secretion.
9. 4. The LH induces the Graafian follicle to burst and eject its eggs into the
fallopian tube,a process called ovulation.
5. Estradiol also stimulates the uterus to prepare for the implantation
nourishment of the foetus likely to arrive after ovulation.
6. Vascularization of uterus increases and the lining of fallopian tubes is
thickened. The ciliary movements also increase and prepare the
fallopian tubes to convey the ovum to the uterus.
LUTEAL PHASE
1.It lasts for 10 days
2.High levels of LH and prolactin hormone stimulate follicular cells of
empty graafian follicle to form yellow colour body called corpus
luteum, which in turn secretes progesterone.
3.Progesterone regulates the hypertropy of endometrium for proper
implantation of foetus.
4.Luteal phase stimulates the endometrial glands to secrete a nutriant fluid
for the foetus, hence it is called the secretory phase.
10. MENSTRUAL PHASE
1.If fertilization does not occur,high concentration of progesterone in
blood inhibits the release of LH.
2.Reduction in LH levels leads to the degeneration of corpus luteum
and a consequent fall in progesterone level in blood.
3.The uterine lining dies due to deficiency of progesterone and is
sloughed off.Blood vessels rupture,causing bleeding,this process
is called the menstrual flow and continues for 3-5 days.
4.The basal part of the endometrium remains intact for next cycle.
5.Lowered levels of progesterone and estradiol due to degeneration
of corpus luteum causes the release of FSH which initiates new
cycle.
11. DESIRABLE FEATURES OF VAGINAL D D S
ďŹ Functionally effective and aesthetically pleasing to the patient.
ďŹ The system must be non-irritant and non-interfering with normal
physiological processes.
ďŹ Sustained release for chronic treatment.
ďŹ Commercially, cost should be low and manufacturing should be easy.
12. INTRODUCTION
ďŹ DEFINITION
ďŹ IUDâs are medicated devices intended to release a small quantity of drug into
uterus in a sustained manner over prolonged period of time.
ďŹ 3 most popular methods:
ďŹ Oral contraceptive pills
ďŹ Condoms or diaphragms
ďŹ Intrauterine device
Methods of
contraception
Pregnancies Births Deaths MBR deaths/
l000 births
P M Total
None 60,000 50,000 12 0.0 12.0 -
Condom or
diaphragm
13,000 10,833 2.5 00 2.5 0.664
Oral pills 100 83 0.0 3.0 3.0 0.060
IUDs 2190 1825 0.44 0.3 0.74 0.015
13. INTRA UTERINE DIVICES (IUDâs)
An Intrauterine Device (IUD) is a small object that is inserted through
the cervix and placed in the uterus to prevent pregnancy.
A small string hangs down from the IUD into the upper part of the vagina.
The IUD is not noticeable during intercourse.
IUDâs can show pharmacological efficacy for about 1-10 years.
M O A :They work by changing the lining of the uterus and fallopian tubes
affecting the movements of eggs and sperm and so that fertilization does
not occur.
14. DEVELOPMENT OF IUDâs
Development of IUDâs began in the 1920s, with the first generation
of IUDâs constructed from silkworm gut and flexible metal wire. Eg-
Grafenberg star and Ota ring.
Fell into disrepute because of the difficulty of insertion, the need for
frequent removal as a result of pain and bleeding.
Subsequently, plastic IUDâs of varying shapes and sizes were made
available.
Various inert, biocompatible, polymeric materials â such as
polyethylene and silicone elastomer â were widely used to construct
IUDâs.
15. ďŽ These devices cause more endometrial compression and myometrial
distension, leading to uterine cramps, bleeding,expulsion of IUDâs.
ďŽ Researchers developed IUDâs in last 30 years with aim - to add
antifertility agents to more tolerated, smaller devices, such as the T-
shaped device, to enhance effectiveness; or antifibrinolytic agents, such
as e-aminocaproic acid and tranexamic acid to larger IUDâs to minimize
the bleeding and pain.
ďŽ Tatum developed a T â shaped device to confirm to the better contours
of uterus. This reduced side effects significantly.
16. ďŽ Zipper 1968 added contraceptive metals (Cu) and Doyle and Clewe
developed progestin â releasing IUDâs.
ďŽ This development initiated a new era of R & D for long term I.U
contraception, leading to generation of recent IUDâsâ the medicated
IUDâs.
ďŽ Copper bearing IUDâs, such as Cu â 7 and progesterone releasing IUDâs
such as Progestasert thus evolved.
18. TYPES
a) Non- medicated IUDâs:
These IUDâs exert their contraceptive action by producing a
sterile inflammatory response in the endometrium by its mechanical
interaction. These do not contain any therapeutic agent.
e.g. ring shaped IUDâs plastic IUDâs, lippes loop, Dalkon shield, Saf-
T-Coil.
b) Medicated IUDâs:
These IUDâs are capable of delivering pharmacologically active
antifertility agents.
e.g. copper bearing IUDâs, progesterone releasing IUDâs.
19. Non â medicated IUDâs
These IUDâs do not contain any therapeutically active agent.
These prominantly make use of metal or plastic rings and coils.
e.g. Dalkon shield, Lippes loop, Saf - T- coil.
Rings of stainless steel have mechanical effects on the uterus leading to
contraception.
Plastic rings also act as mechanical barrier for sperms and eggs so they donât
fuse.
Plastic rings are made from sterile materials such as polyethylene and
polypropylene
20. Non medicated IUDâs have vanished from market.
because of one or more following reasons :
ďŹ Newer devices that are safer and effective.
ďŹ Irregularities in menstrual bleeding.
ďŹ Discomfort and lower patient compliance
ďŹ Cases of pelvic inflammatory diseases (PID).
ďŹ They show higher rates of pregnancies.
23. 1) COPPER BEARING IUDâs
E.g. cu 7
⢠This device uses copper wire wound to
the stem.
⢠The device is made of T shaped
polyethylene plastic.
⢠There are various grades as per the
surface area of the Cu-wire such as
Cu-T-30, Cu-T-200, Cu-T-380
24. ďŹ Cytotoxic
ďŹ Low conc.- Spermatocidal & Spermatodepressive
ďŹ Contraceptive Effectiveness is more.
ďŹ Pregnancy rate âreduced to 5%
ďŹ e.g. cu âT-200, cu-T-30, cu-T-380, Cu-T-220
ďŹ Copper wire thickness â0.2-0.4 mm
25. Mechanism of action
Interfere with
ability of sperm to
pass through
uterine cavity
Thicken cervical
mucus
Interfere with
reproductive process
before ova reach
uterine cavity
Change
endometrial
lining
26. Clinical effectiveness of Cu-T and Cu-7
Pregnancy
rate
Treatment (Months)
Cu â T
Cu â 7
Uterus
Uterine cavity
Copper wine
around plastic T
Thread for insertion or removal of device
Diagram of Cu-T
27. Antifertility Action of Copper
ďŹ In high concentration copper is cytotoxic. It enhance the spermatocidal
and spermato- depressive action of an IUD.
ďŹ Cupric ion (Cu++) is a competitive inhibitor of progesterone and to
lesser effect estrogen.
ďŹ Evoke sterile inflammatory response in the endometrium.
28. Release of Copper from the device
ď The release is linear by chelation, ionization, and corrosion over the
period of 12 years.
ď Release rate is directly proportional to the surface area of exposed Cu.
ď e.g. Cu-T-380A
ď It has a surface area of 380 sq.mm
ď Composed of polyethylene T with 176mg Cu wire on stem and 66.5mg
on the arms.
ď Approved by FDA for 10 year use.
ď The Cu-T-380 Ag IUD differs only at Cu has Ag core that slows the
corrosion rate.
29. Side effects
ďŽ Menstrual problems. About 12% of women have the Copper T
380-A IUD removed because of increased menstrual bleeding or
cramping.
ďŽ Perforation. In 1 out of every 1,000 women, the IUD will get
stuck in or puncture (perforate) the uterus. Although perforation is
rare, it almost always occurs during insertion.
ďŽ Expulsion. About 2% to 10% of IUDâs are expelled from the
uterus. This usually happens in the first few months of use.
Expulsion is more likely when the IUD is inserted right after
childbirth or in a nulliparous woman (a woman who has never
given birth to a child before).
30. 2) HORMONE RELEASING IUDâs (e.g., Progestasert }
ďŽ Doyle and Clewe first initiated the use of hormone releasing IUDâs.
ďŽ Scommegna et al in 1970 carried human testing using conventional IUD
having contraceptive steroids.
ďŽ A T-shaped progesterone releasing IUD having vertical limb embedded
with drug-containing silicone capsule was evolved.
ďŽ Coated with polymer for achieving slower release.
31. ďŹ Objectives
ďŹ Enhance uterine retension
ďŹ Show slowly releasing steroids
ďŹ e.g. Melengestrol acetate.
ďŹ Formulation:
ďŹ Suspension of Progesterone microcrystal ďŽ Silicon medial fluid ďŽ
Ethylene- Vinyl acetate copolymer (EVA)
ďŹ Release rate-65 ďg/ day for one year.
32. Progestesert :
A novel progesterone (pg) releasing IUD.
ďŽ The device has a solid poly EVA (ethyl vinyl acetate) side arms
and a hollow core. The microcrystalline Pg is suspended in the
core in the silicone oil with BaSo4.
ďŽ Dimensions-0.25mm thick, pg is released by diffusion through
rate limiting membrane.
ďŽ Loaded with 38mg of Pg, release rate is 65 mcg/day
ďŽ Approved by USFDA in 1975 for 12 month contraceptive use
ďŽ Preg. rate 1.8/100 for parous and 2.5/100 for nulliparous.
ďŽ Does not inhibit ovulation but interfere with implantation in
endometrium, thickening of cervical mucus.
33. ďŽ Intrauterine administration was compared with oral delivery and
sub-cutanous injection. Progesterone administered I U shows 45
times greater bioavailability than the other 2 routes.
ďŽ Apparently the endometrium tissue is extremely effective for
progesterone absorption.
Advantages :
Increased effectiveness, lower menstrual blood flow, decreased
dysmenorrhea.
Disadvantages :
Need to be replaced yearly, intermenstrual bleeding, ectopic
pregnancies.
35. Antifertility action of progesterone releasing IUDs:
1. They diminish sperm transport through the cervix to the
oviduct by increasing the thickness of the cervical mucous.
2. Steroid releasing devices induce progesteronal changes that
result in endometrial gland atrophy and inhibit further
development of the ova.
3. Endometrial hypermaturation is unfavorable for implantation
of a blastocyst. This is associated with decidual formation
induced by progesterone.
4. Effect of estrogen-progesterone system is related to the
presence of a membrane electrical potential that inhibits the
ovum-endometrium contact before the occurrence of
implantations.
36. Levonorgesterol releasing IUD
ďŽ These carry levonorgesterol releasing device. It is an intrauterine system that has
sleeves of levonorgesterol 52 mg around its stem.
ďŽ It is composed of a polyethylene stem covered by matrix Silastin :LNg (2:1).
ďŽ Releasing 20 mcg/day and lasting for at least 5 years. Initial fast release then at 60 %
drug release rate reduces to 16mcg/day.
ďŽ Suppresses endometrium and ovulation.
ďŽ Also, unlike other IUDs, it may reduce the risk of (PID).
37.
38. Mode of action :
ďŽ Prevents fertilization by damaging or killing sperm and making the
mucus thick and sticky, so sperm can't get through to the uterus.
ďŽ It also keeps endometrium from growing very thick, making lining a
poor place for a fertilized egg to implant and grow.
ďŽ It may relieve irregular menstrual bleeding and cramping.
39. Disadvantages of LNg IUD
ďŽ It may cause noncancerous (benign) growths called ovarian cysts, which
usually go away on their own.
ďŽ It can cause hormonal side effects, such as breast tenderness, mood
swings, headaches, and acne. When side effects do happen, they usually
go away after the first few months.
40. Contraindications
⢠pregnancy
⢠puerperal sepsis or immediate post septic
abortion
⢠distorted uterine cavity (congenital or acquired)
⢠unexplained vaginal bleeding
⢠suspected genital malignancy
⢠genital tuberculosis
⢠active Pelvic Inflammatory Disease (PID)
41. WHAT ARE THE ADVANTAGES OF AN
IUD?
â˘Copper T 380 A IUD (ParaGard) is effective for at least
12 yeCopper T IUD (ParaGard) and Levonorgestetrel IUD (Mirena) are the
two most effective reversible methods of birth control.
ďˇOnly 1 out of 100 women using a Copper T for 12 years will become
pregnant.
ďˇThe copper IUD prevents ectopic pregnancies.
ďˇThis contraceptive is very cost effective (inexpensive) over time.
ďˇUse of an IUD is convenient, safe & private.
42. ďˇAll you have to do is check for the strings each month.
ďˇThe ParaGard IUD may be used by women who cannot use
estrogenâcontaining birth control pills, patches or vaginal ring
including breastfeeding women.
ďˇThe IUD may be inserted immediately following the delivery
of a baby or immediately after an abortion.
ďˇSome studies of IUDs have shown a decreased risk for uterine
cancer. There is also some evidence that IUDs protect against
cervical cancer.
43. WHAT ARE THE DISADVANTAGES OF AN
IUD?
ďŹ There may be cramping, pain or spotting after insertion.
ďŹ The number of bleeding days is slightly higher than normal
and you may have somewhat increased menstrual
cramping. If your bleeding pattern is bothersome to you,
contact your doctor. There are medications which may give
you a more acceptable pattern of bleeding and cramping.
ďŹ The IUD provides no protection against sexually
transmitted infections. Use condoms if there is any risk.
ďŹ There is a higher initial cost of insertion. However, after 2
years, it is the most cost-effective contraceptive method.
44. â˘The IUD must be inserted by a doctor, nurse practitioner, nurse midwife or
physicianâs assistant.
â˘A very small percentage of women are allergic to copper.
⢠A small percentage of IUDs may be expelled by a womanâs body within
the first few months due to an improper fit.
45. QUESTIONS
1. Write a note on medicated IUDâs
2. Discuss the development of copper IUDâs & hormone releasing IUDâs
3. Write a note on copper IUDâs
4. Write a note on hormone releasing IUDâs
5. Write a note on contraindications of IUDâs
46. Reference
ďŹ Y.W. Chien. Novel Drug Delivery System, 2nd edition,
Marcel Decker , page no.- 585-630
ďŹ Advanced in controlled & novel drug delivery-
N.K.Jain, page no.- 112-123
ďŹ Remington-the science & practice of pharmacy
vol.1&2.
ďŹ Internet source